Chemicals

Showing 19501–19650 of 41137 results

  • FFN-102 is a fluorescent false neurotransmitter (FFN) that is a substrate for the dopamine transporter (DAT) and vesicular monoamine transporter 2 (VMAT2).{38320} It is a pH-dependent fluorescent probe that labels dopamine cell bodies, axons, and presynaptic terminals. It can also be used to monitor dopamine exocytosis.{38319} It has a pKa of 6.2 and displays pH-dependent excitation spectra of 340 and 370 nm at pH 5 and 7.4, respectively, which correspond to vesicular and cytoplasmic pH values.{38320} The emission spectrum of FFN-102 is pH-independent at 453 nm, but the intensity of emission is pH-dependent with a higher intensity at a pH of 7.4. FFN-102 inhibits DAT (13.6% at a concentration of 10 µM) and the serotonin (5-HT) receptor subtype 5-HT2c (Ki = ~3 µM) but does not bind to 37 other central nervous system receptors and transporters, including dopamine receptors, up to a concentration of 10 µM.{38320}  

     

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    Cayman
    SKU:21458 -

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  • Hypoxia-inducible factor (HIF) prolyl hydroxylase (PHD) enzymes act as central gatekeepers of post-transcriptional and transcriptional adaptation to hypoxia, oxidative stress, and excitotoxicity. FG-2216 is an orally active PHD2 inhibitor (IC50 = 3.9 µM) that stabilizes HIF-α.{30802} It has been shown to reversibly stimulate erythropoietin secretion at 100 µM in vitro and to increase hematocrit, red blood cell count, and hemoglobin levels at 50 mg/kg in mice.{30802,25021}  

     

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  • Hypoxia-inducible factor (HIF) prolyl hydroxylase (PHD) enzymes act as central gatekeepers of post-transcriptional and transcriptional adaptation to hypoxia, oxidative stress, and excitotoxicity. FG-2216 is an orally active PHD2 inhibitor (IC50 = 3.9 µM) that stabilizes HIF-α.{30802} It has been shown to reversibly stimulate erythropoietin secretion at 100 µM in vitro and to increase hematocrit, red blood cell count, and hemoglobin levels at 50 mg/kg in mice.{30802,25021}  

     

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  • Hypoxia-inducible factor (HIF) prolyl hydroxylase (PHD) enzymes act as central gatekeepers of post-transcriptional and transcriptional adaptation to hypoxia, oxidative stress, and excitotoxicity. FG-2216 is an orally active PHD2 inhibitor (IC50 = 3.9 µM) that stabilizes HIF-α.{30802} It has been shown to reversibly stimulate erythropoietin secretion at 100 µM in vitro and to increase hematocrit, red blood cell count, and hemoglobin levels at 50 mg/kg in mice.{30802,25021}  

     

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    Cayman
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  • Hypoxia-inducible factor (HIF) prolyl hydroxylase (PHD) enzymes act as central gatekeepers of post-transcriptional and transcriptional adaptation to hypoxia, oxidative stress, and excitotoxicity. FG-2216 is an orally active PHD2 inhibitor (IC50 = 3.9 µM) that stabilizes HIF-α.{30802} It has been shown to reversibly stimulate erythropoietin secretion at 100 µM in vitro and to increase hematocrit, red blood cell count, and hemoglobin levels at 50 mg/kg in mice.{30802,25021}  

     

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    Cayman
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  • The hypoxia-inducible factor (HIF) pathway alters gene expression in response to low oxygen tension. Under normoxic conditions, HIF-specific prolyl hydroxylases (HIF-PHs) initiate the degradation of oxygen-sensitive HIF isoforms. As 2-oxoglutarate (2-OG) is a required co-factor for HIF-PH activity, analogs of 2-OG may inhibit HIF-PH and prevent HIF turnover.{25022} FG-4592 is an analog of 2-OG that has been developed as an inhibitor of HIF-PHs. While little has been published regarding the actions of this compound, similar HIF-PH inhibitors suppress HIF degradation and in this way induce erythropoietin expression, promoting erythropoiesis or preventing anemia in vivo.{25021}  

     

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  • The hypoxia-inducible factor (HIF) pathway alters gene expression in response to low oxygen tension. Under normoxic conditions, HIF-specific prolyl hydroxylases (HIF-PHs) initiate the degradation of oxygen-sensitive HIF isoforms. As 2-oxoglutarate (2-OG) is a required co-factor for HIF-PH activity, analogs of 2-OG may inhibit HIF-PH and prevent HIF turnover.{25022} FG-4592 is an analog of 2-OG that has been developed as an inhibitor of HIF-PHs. While little has been published regarding the actions of this compound, similar HIF-PH inhibitors suppress HIF degradation and in this way induce erythropoietin expression, promoting erythropoiesis or preventing anemia in vivo.{25021}  

     

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    Cayman
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  • The hypoxia-inducible factor (HIF) pathway alters gene expression in response to low oxygen tension. Under normoxic conditions, HIF-specific prolyl hydroxylases (HIF-PHs) initiate the degradation of oxygen-sensitive HIF isoforms. As 2-oxoglutarate (2-OG) is a required co-factor for HIF-PH activity, analogs of 2-OG may inhibit HIF-PH and prevent HIF turnover.{25022} FG-4592 is an analog of 2-OG that has been developed as an inhibitor of HIF-PHs. While little has been published regarding the actions of this compound, similar HIF-PH inhibitors suppress HIF degradation and in this way induce erythropoietin expression, promoting erythropoiesis or preventing anemia in vivo.{25021}  

     

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    Cayman
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  • The hypoxia-inducible factor (HIF) pathway alters gene expression in response to low oxygen tension. Under normoxic conditions, HIF-specific prolyl hydroxylases (HIF-PHs) initiate the degradation of oxygen-sensitive HIF isoforms. As 2-oxoglutarate (2-OG) is a required co-factor for HIF-PH activity, analogs of 2-OG may inhibit HIF-PH and prevent HIF turnover.{25022} FG-4592 is an analog of 2-OG that has been developed as an inhibitor of HIF-PHs. While little has been published regarding the actions of this compound, similar HIF-PH inhibitors suppress HIF degradation and in this way induce erythropoietin expression, promoting erythropoiesis or preventing anemia in vivo.{25021}  

     

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  • FG-7142 is a benzodiazepine receptor ligand with anxiogenic and proconvulsant properties.{48712} It increases benzodiazepine receptor ligand binding and GABA-dependent chloride uptake in primary chick cerebral cortical neurons when used at a concentration of 1 μM. FG-7142 (5 mg/kg) decreases pinning of the other animal and increases avoiding behavior in rats, an effect that can be prevented by the benzodiazepine receptor antagonist Ro 15-1788 (flumazenil; Item No. 14252).{48713} It reduces the infused pentylenetetrazol (PTZ; Item No. 18682) seizure threshold and induces generalized seizures in mice when administered at doses of 10 and 40 mg/kg, respectively.{48714} FG-7142 (3.75, 7.5, and 15 mg/kg, i.p.) also decreases food and water intake, eating rate, and time spent in the open arms of the elevated plus maze in female rats.{48715}  

     

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    Cayman
    SKU:29183 - 100 mg

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  • FG-7142 is a benzodiazepine receptor ligand with anxiogenic and proconvulsant properties.{48712} It increases benzodiazepine receptor ligand binding and GABA-dependent chloride uptake in primary chick cerebral cortical neurons when used at a concentration of 1 μM. FG-7142 (5 mg/kg) decreases pinning of the other animal and increases avoiding behavior in rats, an effect that can be prevented by the benzodiazepine receptor antagonist Ro 15-1788 (flumazenil; Item No. 14252).{48713} It reduces the infused pentylenetetrazol (PTZ; Item No. 18682) seizure threshold and induces generalized seizures in mice when administered at doses of 10 and 40 mg/kg, respectively.{48714} FG-7142 (3.75, 7.5, and 15 mg/kg, i.p.) also decreases food and water intake, eating rate, and time spent in the open arms of the elevated plus maze in female rats.{48715}  

     

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    Cayman
    SKU:29183 - 50 mg

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  • FGF401 is an inhibitor of FGF receptor 4 (FGFR4; IC50 = 1.9 nM).{43774} It inhibits proliferation of Huh7 carcinoma cells with an IC50 value of 12 nM. FGF401 induces bile acid synthesis in dogs, increasing plasma and fecal levels of bile acids when administered at a dose of 45 mg/kg per day for four weeks.{43775} It also decreases serum cholesterol when administered at doses ranging from 5 to 45 mg/kg per day.  

     

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    Cayman
    SKU:23029 - 1 mg

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  • FGF401 is an inhibitor of FGF receptor 4 (FGFR4; IC50 = 1.9 nM).{43774} It inhibits proliferation of Huh7 carcinoma cells with an IC50 value of 12 nM. FGF401 induces bile acid synthesis in dogs, increasing plasma and fecal levels of bile acids when administered at a dose of 45 mg/kg per day for four weeks.{43775} It also decreases serum cholesterol when administered at doses ranging from 5 to 45 mg/kg per day.  

     

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    Cayman
    SKU:23029 - 10 mg

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  • FGF401 is an inhibitor of FGF receptor 4 (FGFR4; IC50 = 1.9 nM).{43774} It inhibits proliferation of Huh7 carcinoma cells with an IC50 value of 12 nM. FGF401 induces bile acid synthesis in dogs, increasing plasma and fecal levels of bile acids when administered at a dose of 45 mg/kg per day for four weeks.{43775} It also decreases serum cholesterol when administered at doses ranging from 5 to 45 mg/kg per day.  

     

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    Cayman
    SKU:23029 - 25 mg

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  • FGF401 is an inhibitor of FGF receptor 4 (FGFR4; IC50 = 1.9 nM).{43774} It inhibits proliferation of Huh7 carcinoma cells with an IC50 value of 12 nM. FGF401 induces bile acid synthesis in dogs, increasing plasma and fecal levels of bile acids when administered at a dose of 45 mg/kg per day for four weeks.{43775} It also decreases serum cholesterol when administered at doses ranging from 5 to 45 mg/kg per day.  

     

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    Cayman
    SKU:23029 - 5 mg

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  • FGFR-IN-1 is an inhibitor of FGF receptor 4 (FGFR4; IC50 = 1.3 nM).{43774} It is selective for FGFR4 over FGFR1 and a panel of 36 kinases (IC50s = >10 µM for all). It inhibits proliferation of Hep3B and Huh7 hepatic cancer cells with IC50 values of 1.1 and 2.5 nM, respectively. FGFR-IN-1 reduces tumor growth by 62.7 and 70.8% in a Huh7 mouse xenograft model when administered at doses of 30 and 100 mg/kg per day, respectively.  

     

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    Cayman
    SKU:21342 -

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  • FGFR-IN-1 is an inhibitor of FGF receptor 4 (FGFR4; IC50 = 1.3 nM).{43774} It is selective for FGFR4 over FGFR1 and a panel of 36 kinases (IC50s = >10 µM for all). It inhibits proliferation of Hep3B and Huh7 hepatic cancer cells with IC50 values of 1.1 and 2.5 nM, respectively. FGFR-IN-1 reduces tumor growth by 62.7 and 70.8% in a Huh7 mouse xenograft model when administered at doses of 30 and 100 mg/kg per day, respectively.  

     

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    Cayman
    SKU:21342 -

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  • FGFR-IN-1 is an inhibitor of FGF receptor 4 (FGFR4; IC50 = 1.3 nM).{43774} It is selective for FGFR4 over FGFR1 and a panel of 36 kinases (IC50s = >10 µM for all). It inhibits proliferation of Hep3B and Huh7 hepatic cancer cells with IC50 values of 1.1 and 2.5 nM, respectively. FGFR-IN-1 reduces tumor growth by 62.7 and 70.8% in a Huh7 mouse xenograft model when administered at doses of 30 and 100 mg/kg per day, respectively.  

     

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    Cayman
    SKU:21342 -

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  • FGFR-IN-1 is an inhibitor of FGF receptor 4 (FGFR4; IC50 = 1.3 nM).{43774} It is selective for FGFR4 over FGFR1 and a panel of 36 kinases (IC50s = >10 µM for all). It inhibits proliferation of Hep3B and Huh7 hepatic cancer cells with IC50 values of 1.1 and 2.5 nM, respectively. FGFR-IN-1 reduces tumor growth by 62.7 and 70.8% in a Huh7 mouse xenograft model when administered at doses of 30 and 100 mg/kg per day, respectively.  

     

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    Cayman
    SKU:21342 -

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  • FGIN-1-27 is an indoleacetamide that acts as a high affinity agonist of the 18 kDa translocator protein (TSPO; previously called the peripheral benzodiazepine receptor) with a Ki value of 5 nM.{30265} It can enhance steroidogenesis of neuroactive steroids such as allopregnanolone (Item No. 16930).{30265} Through this action, FGIN-1-27 indirectly potentiates GABAA receptor signaling to produce anticonvulsant, anxiolytic, and sedative activity in both animal and clinical models.{30265}  

     

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  • FGIN-1-27 is an indoleacetamide that acts as a high affinity agonist of the 18 kDa translocator protein (TSPO; previously called the peripheral benzodiazepine receptor) with a Ki value of 5 nM.{30265} It can enhance steroidogenesis of neuroactive steroids such as allopregnanolone (Item No. 16930).{30265} Through this action, FGIN-1-27 indirectly potentiates GABAA receptor signaling to produce anticonvulsant, anxiolytic, and sedative activity in both animal and clinical models.{30265}  

     

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    Cayman
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  • FGIN-1-27 is an indoleacetamide that acts as a high affinity agonist of the 18 kDa translocator protein (TSPO; previously called the peripheral benzodiazepine receptor) with a Ki value of 5 nM.{30265} It can enhance steroidogenesis of neuroactive steroids such as allopregnanolone (Item No. 16930).{30265} Through this action, FGIN-1-27 indirectly potentiates GABAA receptor signaling to produce anticonvulsant, anxiolytic, and sedative activity in both animal and clinical models.{30265}  

     

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    Cayman
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  • FGIN-1-27 is an indoleacetamide that acts as a high affinity agonist of the 18 kDa translocator protein (TSPO; previously called the peripheral benzodiazepine receptor) with a Ki value of 5 nM.{30265} It can enhance steroidogenesis of neuroactive steroids such as allopregnanolone (Item No. 16930).{30265} Through this action, FGIN-1-27 indirectly potentiates GABAA receptor signaling to produce anticonvulsant, anxiolytic, and sedative activity in both animal and clinical models.{30265}  

     

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  • FH535 is an inhibitor of β-catenin/Tcf-mediated transcription and an antagonist of ligand-dependent activation of PPARγ and PPARδ.{15982} At 15 µM, FH535 blocks the recruitment of β-catenin and GRIP1 to PPARγ and PPARδ.{15982} Presumably through these actions, FH535 is selectively toxic to some carcinoma cell lines expressing the Wnt/β-catenin pathway.{15982} FH535 is used to study the role of Wnt/β-catenin pathway in various cancer cell lines.{30755,30756,30757}  

     

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  • FH535 is an inhibitor of β-catenin/Tcf-mediated transcription and an antagonist of ligand-dependent activation of PPARγ and PPARδ.{15982} At 15 µM, FH535 blocks the recruitment of β-catenin and GRIP1 to PPARγ and PPARδ.{15982} Presumably through these actions, FH535 is selectively toxic to some carcinoma cell lines expressing the Wnt/β-catenin pathway.{15982} FH535 is used to study the role of Wnt/β-catenin pathway in various cancer cell lines.{30755,30756,30757}  

     

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  • FH535 is an inhibitor of β-catenin/Tcf-mediated transcription and an antagonist of ligand-dependent activation of PPARγ and PPARδ.{15982} At 15 µM, FH535 blocks the recruitment of β-catenin and GRIP1 to PPARγ and PPARδ.{15982} Presumably through these actions, FH535 is selectively toxic to some carcinoma cell lines expressing the Wnt/β-catenin pathway.{15982} FH535 is used to study the role of Wnt/β-catenin pathway in various cancer cell lines.{30755,30756,30757}  

     

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  • FH535 is an inhibitor of β-catenin/Tcf-mediated transcription and an antagonist of ligand-dependent activation of PPARγ and PPARδ.{15982} At 15 µM, FH535 blocks the recruitment of β-catenin and GRIP1 to PPARγ and PPARδ.{15982} Presumably through these actions, FH535 is selectively toxic to some carcinoma cell lines expressing the Wnt/β-catenin pathway.{15982} FH535 is used to study the role of Wnt/β-catenin pathway in various cancer cell lines.{30755,30756,30757}  

     

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  • Fialuridine (FIAU) is a nucleoside analog with antiviral activity. It inhibits thymidine kinases from herpes simplex virus types 1 and 2 with Ki values of 0.14 and 0.95 µM, respectively, while blocking green monkey Vero cell thymidine kinase less effectively (Ki = 53 µM).{26079} FIAU blocks DNA synthesis in human cytomegalovirus and hepatitis B, as well as herpes simplex.{26078,26080,26081} Notably, while FIAU has few adverse effects in several mammals, it causes mitochondrial toxicity leading to liver damage and death in humans.{26082}  

     

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  • Fialuridine (FIAU) is a nucleoside analog with antiviral activity. It inhibits thymidine kinases from herpes simplex virus types 1 and 2 with Ki values of 0.14 and 0.95 µM, respectively, while blocking green monkey Vero cell thymidine kinase less effectively (Ki = 53 µM).{26079} FIAU blocks DNA synthesis in human cytomegalovirus and hepatitis B, as well as herpes simplex.{26078,26080,26081} Notably, while FIAU has few adverse effects in several mammals, it causes mitochondrial toxicity leading to liver damage and death in humans.{26082}  

     

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  • Fialuridine (FIAU) is a nucleoside analog with antiviral activity. It inhibits thymidine kinases from herpes simplex virus types 1 and 2 with Ki values of 0.14 and 0.95 µM, respectively, while blocking green monkey Vero cell thymidine kinase less effectively (Ki = 53 µM).{26079} FIAU blocks DNA synthesis in human cytomegalovirus and hepatitis B, as well as herpes simplex.{26078,26080,26081} Notably, while FIAU has few adverse effects in several mammals, it causes mitochondrial toxicity leading to liver damage and death in humans.{26082}  

     

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    Cayman
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  • Fialuridine (FIAU) is a nucleoside analog with antiviral activity. It inhibits thymidine kinases from herpes simplex virus types 1 and 2 with Ki values of 0.14 and 0.95 µM, respectively, while blocking green monkey Vero cell thymidine kinase less effectively (Ki = 53 µM).{26079} FIAU blocks DNA synthesis in human cytomegalovirus and hepatitis B, as well as herpes simplex.{26078,26080,26081} Notably, while FIAU has few adverse effects in several mammals, it causes mitochondrial toxicity leading to liver damage and death in humans.{26082}  

     

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  • Fidarestat is an aldose reductase inhibitor (IC50 = 0.026 μM using human recombinant enzyme) that also inhibits aldo-keto reductase family 1 member B10 (AKR1B10; IC50 = 33 μM using human recombinant enzyme).{38790} It decreases sorbitol and myo-inositol levels in the sciatic nerve of rats with diabetes induced by streptozotocin (STZ; Item No. 13104) when administered at a dose of 2 mg/kg per day.{38791} Fidarestat (2 mg/kg per day) decreases nerve fiber abnormalities and reverses slowing of motor nerve conduction velocity (MNCV) in an STZ-induced diabetic rat model of peripheral neuropathy. It decreases the pain threshold in STZ-induced diabetic mice that overexpress human aldose reductase when administered at 4 mg/kg per day.{38792} Fidarestat (50 mg/kg per day) decreases metastasis in a KM20 human colorectal cancer mouse xenograft model.{38793}  

     

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    SKU:21756 -

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  • Fidarestat is an aldose reductase inhibitor (IC50 = 0.026 μM using human recombinant enzyme) that also inhibits aldo-keto reductase family 1 member B10 (AKR1B10; IC50 = 33 μM using human recombinant enzyme).{38790} It decreases sorbitol and myo-inositol levels in the sciatic nerve of rats with diabetes induced by streptozotocin (STZ; Item No. 13104) when administered at a dose of 2 mg/kg per day.{38791} Fidarestat (2 mg/kg per day) decreases nerve fiber abnormalities and reverses slowing of motor nerve conduction velocity (MNCV) in an STZ-induced diabetic rat model of peripheral neuropathy. It decreases the pain threshold in STZ-induced diabetic mice that overexpress human aldose reductase when administered at 4 mg/kg per day.{38792} Fidarestat (50 mg/kg per day) decreases metastasis in a KM20 human colorectal cancer mouse xenograft model.{38793}  

     

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    Cayman
    SKU:21756 -

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  • Fidarestat is an aldose reductase inhibitor (IC50 = 0.026 μM using human recombinant enzyme) that also inhibits aldo-keto reductase family 1 member B10 (AKR1B10; IC50 = 33 μM using human recombinant enzyme).{38790} It decreases sorbitol and myo-inositol levels in the sciatic nerve of rats with diabetes induced by streptozotocin (STZ; Item No. 13104) when administered at a dose of 2 mg/kg per day.{38791} Fidarestat (2 mg/kg per day) decreases nerve fiber abnormalities and reverses slowing of motor nerve conduction velocity (MNCV) in an STZ-induced diabetic rat model of peripheral neuropathy. It decreases the pain threshold in STZ-induced diabetic mice that overexpress human aldose reductase when administered at 4 mg/kg per day.{38792} Fidarestat (50 mg/kg per day) decreases metastasis in a KM20 human colorectal cancer mouse xenograft model.{38793}  

     

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    Cayman
    SKU:21756 -

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  • Fidaxomycin is a natural macrocyclic antibiotic that inhibits RNA polymerase with selectivity for Gram-positive bacteria over Gram-negative bacteria (IC50s = 0.4 and 6 μM, respectively).{25092} It has potent antibacterial activity against most Gram-positive bacteria and effectively targets the Gram-positive C. difficile (MIC = 12 ng/ml).{25092} Orally administered fidaxomycin exhibits minimal systemic bioavailability resulting in maximal gastrointestinal tract distribution.{25092} Fidaxomycin is effective in clearing C. difficile infections while sparing Gram-negative bacteria in the gut.{25090,25089}  

     

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  • Fidaxomycin is a natural macrocyclic antibiotic that inhibits RNA polymerase with selectivity for Gram-positive bacteria over Gram-negative bacteria (IC50s = 0.4 and 6 μM, respectively).{25092} It has potent antibacterial activity against most Gram-positive bacteria and effectively targets the Gram-positive C. difficile (MIC = 12 ng/ml).{25092} Orally administered fidaxomycin exhibits minimal systemic bioavailability resulting in maximal gastrointestinal tract distribution.{25092} Fidaxomycin is effective in clearing C. difficile infections while sparing Gram-negative bacteria in the gut.{25090,25089}  

     

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  • Fidaxomycin is a natural macrocyclic antibiotic that inhibits RNA polymerase with selectivity for Gram-positive bacteria over Gram-negative bacteria (IC50s = 0.4 and 6 μM, respectively).{25092} It has potent antibacterial activity against most Gram-positive bacteria and effectively targets the Gram-positive C. difficile (MIC = 12 ng/ml).{25092} Orally administered fidaxomycin exhibits minimal systemic bioavailability resulting in maximal gastrointestinal tract distribution.{25092} Fidaxomycin is effective in clearing C. difficile infections while sparing Gram-negative bacteria in the gut.{25090,25089}  

     

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  • FIIN-2 is an irreversible FGFR inhibitor with IC50 values of 3.09, 4.3, 27, and 45.3 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively.{32873} It has been shown to inhibit cell proliferation of transformed Ba/F3 cell lines and demonstrates antiproliferative activity in cells dependent upon the gatekeeper mutants of FGFR1 or FGFR2.{32873} By inhibiting FGFR in a zebrafish developmental model, FIIN-2 caused mild to severe alterations in tail morphogenesis similar to the phenotypes reported following genetic knockdown of FGFR.{32873}  

     

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    SKU:19837 -

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  • FIIN-2 is an irreversible FGFR inhibitor with IC50 values of 3.09, 4.3, 27, and 45.3 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively.{32873} It has been shown to inhibit cell proliferation of transformed Ba/F3 cell lines and demonstrates antiproliferative activity in cells dependent upon the gatekeeper mutants of FGFR1 or FGFR2.{32873} By inhibiting FGFR in a zebrafish developmental model, FIIN-2 caused mild to severe alterations in tail morphogenesis similar to the phenotypes reported following genetic knockdown of FGFR.{32873}  

     

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    SKU:19837 -

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  • FIIN-2 is an irreversible FGFR inhibitor with IC50 values of 3.09, 4.3, 27, and 45.3 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively.{32873} It has been shown to inhibit cell proliferation of transformed Ba/F3 cell lines and demonstrates antiproliferative activity in cells dependent upon the gatekeeper mutants of FGFR1 or FGFR2.{32873} By inhibiting FGFR in a zebrafish developmental model, FIIN-2 caused mild to severe alterations in tail morphogenesis similar to the phenotypes reported following genetic knockdown of FGFR.{32873}  

     

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    SKU:19837 -

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  • FIIN-2 is an irreversible FGFR inhibitor with IC50 values of 3.09, 4.3, 27, and 45.3 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively.{32873} It has been shown to inhibit cell proliferation of transformed Ba/F3 cell lines and demonstrates antiproliferative activity in cells dependent upon the gatekeeper mutants of FGFR1 or FGFR2.{32873} By inhibiting FGFR in a zebrafish developmental model, FIIN-2 caused mild to severe alterations in tail morphogenesis similar to the phenotypes reported following genetic knockdown of FGFR.{32873}  

     

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    SKU:19837 -

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  • FIIN-3 is an inhibitor of FGF receptors (FGFRs; IC50s = 13, 21, 31, and 35 nM for recombinant FGFR1-4, respectively).{32873} It is selective for FGFRs over a panel of 456 kinases at a concentration of 1 μM, however, it does inhibit EGFR (IC50 = 204 nM). FIIN-3 inhibits growth of Ba/F3 cells that are dependent on the kinase activity of wild-type FGFR1-4 as well as gatekeeper mutant FGFR2 and FGFR3 (EC50s = TEL/V564M-dependent Ba/F3 cells. FIIN-3 also inhibits growth in a panel of cancer cell lines (EC50s = 1.4-499 nM).  

     

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    SKU:20709 -

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  • FIIN-3 is an inhibitor of FGF receptors (FGFRs; IC50s = 13, 21, 31, and 35 nM for recombinant FGFR1-4, respectively).{32873} It is selective for FGFRs over a panel of 456 kinases at a concentration of 1 μM, however, it does inhibit EGFR (IC50 = 204 nM). FIIN-3 inhibits growth of Ba/F3 cells that are dependent on the kinase activity of wild-type FGFR1-4 as well as gatekeeper mutant FGFR2 and FGFR3 (EC50s = TEL/V564M-dependent Ba/F3 cells. FIIN-3 also inhibits growth in a panel of cancer cell lines (EC50s = 1.4-499 nM).  

     

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    Cayman
    SKU:20709 -

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  • FIIN-3 is an inhibitor of FGF receptors (FGFRs; IC50s = 13, 21, 31, and 35 nM for recombinant FGFR1-4, respectively).{32873} It is selective for FGFRs over a panel of 456 kinases at a concentration of 1 μM, however, it does inhibit EGFR (IC50 = 204 nM). FIIN-3 inhibits growth of Ba/F3 cells that are dependent on the kinase activity of wild-type FGFR1-4 as well as gatekeeper mutant FGFR2 and FGFR3 (EC50s = TEL/V564M-dependent Ba/F3 cells. FIIN-3 also inhibits growth in a panel of cancer cell lines (EC50s = 1.4-499 nM).  

     

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    Cayman
    SKU:20709 -

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  • FIIN-3 is an inhibitor of FGF receptors (FGFRs; IC50s = 13, 21, 31, and 35 nM for recombinant FGFR1-4, respectively).{32873} It is selective for FGFRs over a panel of 456 kinases at a concentration of 1 μM, however, it does inhibit EGFR (IC50 = 204 nM). FIIN-3 inhibits growth of Ba/F3 cells that are dependent on the kinase activity of wild-type FGFR1-4 as well as gatekeeper mutant FGFR2 and FGFR3 (EC50s = TEL/V564M-dependent Ba/F3 cells. FIIN-3 also inhibits growth in a panel of cancer cell lines (EC50s = 1.4-499 nM).  

     

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    SKU:20709 -

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  • Filgotinib is a JAK1 inhibitor (IC50 = 10 nM).{30750} It is selective for JAK1 over JAK3 (IC50 = 810 nM) but also inhibits JAK2 and tyrosine kinase 2 (Tyk2; IC50s = 28 and 116 nM, respectively), as well as Abl, FLT1, -3, and -4, FMS, Mer, and TBK1 activity by greater than 35% in a panel of 177 tyrosine kinases at 1 µM. Filgotinib inhibits IL-6-induced phosphorylation of STAT1 in CD4+ T cells with an IC50 value of 629 nM in isolated human whole blood. It reduces hind paw macrophage and T cell infiltration and bone erosion in a rat model of collagen-induced arthritis when administered at doses ranging from 0.1 to 30 mg/kg per day for 15 days.  

     

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  • Filgotinib is a JAK1 inhibitor (IC50 = 10 nM).{30750} It is selective for JAK1 over JAK3 (IC50 = 810 nM) but also inhibits JAK2 and tyrosine kinase 2 (Tyk2; IC50s = 28 and 116 nM, respectively), as well as Abl, FLT1, -3, and -4, FMS, Mer, and TBK1 activity by greater than 35% in a panel of 177 tyrosine kinases at 1 µM. Filgotinib inhibits IL-6-induced phosphorylation of STAT1 in CD4+ T cells with an IC50 value of 629 nM in isolated human whole blood. It reduces hind paw macrophage and T cell infiltration and bone erosion in a rat model of collagen-induced arthritis when administered at doses ranging from 0.1 to 30 mg/kg per day for 15 days.  

     

    Brand:
    Cayman
    SKU:-

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  • Filgotinib is a JAK1 inhibitor (IC50 = 10 nM).{30750} It is selective for JAK1 over JAK3 (IC50 = 810 nM) but also inhibits JAK2 and tyrosine kinase 2 (Tyk2; IC50s = 28 and 116 nM, respectively), as well as Abl, FLT1, -3, and -4, FMS, Mer, and TBK1 activity by greater than 35% in a panel of 177 tyrosine kinases at 1 µM. Filgotinib inhibits IL-6-induced phosphorylation of STAT1 in CD4+ T cells with an IC50 value of 629 nM in isolated human whole blood. It reduces hind paw macrophage and T cell infiltration and bone erosion in a rat model of collagen-induced arthritis when administered at doses ranging from 0.1 to 30 mg/kg per day for 15 days.  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Filgotinib is a JAK1 inhibitor (IC50 = 10 nM).{30750} It is selective for JAK1 over JAK3 (IC50 = 810 nM) but also inhibits JAK2 and tyrosine kinase 2 (Tyk2; IC50s = 28 and 116 nM, respectively), as well as Abl, FLT1, -3, and -4, FMS, Mer, and TBK1 activity by greater than 35% in a panel of 177 tyrosine kinases at 1 µM. Filgotinib inhibits IL-6-induced phosphorylation of STAT1 in CD4+ T cells with an IC50 value of 629 nM in isolated human whole blood. It reduces hind paw macrophage and T cell infiltration and bone erosion in a rat model of collagen-induced arthritis when administered at doses ranging from 0.1 to 30 mg/kg per day for 15 days.  

     

    Brand:
    Cayman
    SKU:-

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  • Filgotinib-d4 is intended for use as an internal standard for the quantification of filgotinib (Item No. 17669) by GC- or LC-MS. Filgotinib is a JAK1 inhibitor (IC50 = 10 nM).{30750} It is selective for JAK1 over JAK3 (IC50 = 810 nM) but also inhibits JAK2 and tyrosine kinase 2 (Tyk2; IC50s = 28 and 116 nM, respectively), as well as Abl, FLT1, -3 and -4, FMS, Mer, and TBK1 activity by greater than 35% in a panel of 177 tyrosine kinases at 1 µM. Filgotinib inhibits IL-6-induced phosphorylation of STAT1 in CD4+ T cells with an IC50 value of 629 nM in isolated human whole blood. It reduces hind paw macrophage and T cell infiltration and bone erosion in a rat model of collagen-induced arthritis when administered at doses ranging from 0.1 to 30 mg/kg per day for 15 days.  

     

    Brand:
    Cayman
    SKU:28875 - 1 mg

    Available on backorder

  • Filgotinib-d4 is intended for use as an internal standard for the quantification of filgotinib (Item No. 17669) by GC- or LC-MS. Filgotinib is a JAK1 inhibitor (IC50 = 10 nM).{30750} It is selective for JAK1 over JAK3 (IC50 = 810 nM) but also inhibits JAK2 and tyrosine kinase 2 (Tyk2; IC50s = 28 and 116 nM, respectively), as well as Abl, FLT1, -3 and -4, FMS, Mer, and TBK1 activity by greater than 35% in a panel of 177 tyrosine kinases at 1 µM. Filgotinib inhibits IL-6-induced phosphorylation of STAT1 in CD4+ T cells with an IC50 value of 629 nM in isolated human whole blood. It reduces hind paw macrophage and T cell infiltration and bone erosion in a rat model of collagen-induced arthritis when administered at doses ranging from 0.1 to 30 mg/kg per day for 15 days.  

     

    Brand:
    Cayman
    SKU:28875 - 5 mg

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  • Filipin complex is a neutral polyene originally isolated from S. filipinensis with antifungal activity.{42119} It inhibits cell growth as well as mitochondrial terminal electron transport in S. cerevisiae when used at a concentration of 135 µg/ml. Filipin complex binds to various sterols, particularly 24α-methyl cholesterol (Item no. 17344), 24α-ethyl cholesterol (Item no. 11756), and cholesterol, in aqueous solutions and in fungal cell membranes when used at a concentration of 50 µg/ml, inducing membrane pit formation and leakage of cell contents.{42120,9103,42106} It is a fluorescent compound that has been used to label sterols within biological structures for imaging.{9103,8625,42104,42105} Filipin complex displays excitation/emission maxima of 338/480 nm, respectively.  

     

    Brand:
    Cayman
    SKU:25073 - 25 mg

    Available on backorder

  • Filipin complex is a neutral polyene originally isolated from S. filipinensis with antifungal activity.{42119} It inhibits cell growth as well as mitochondrial terminal electron transport in S. cerevisiae when used at a concentration of 135 µg/ml. Filipin complex binds to various sterols, particularly 24α-methyl cholesterol (Item no. 17344), 24α-ethyl cholesterol (Item no. 11756), and cholesterol, in aqueous solutions and in fungal cell membranes when used at a concentration of 50 µg/ml, inducing membrane pit formation and leakage of cell contents.{42120,9103,42106} It is a fluorescent compound that has been used to label sterols within biological structures for imaging.{9103,8625,42104,42105} Filipin complex displays excitation/emission maxima of 338/480 nm, respectively.  

     

    Brand:
    Cayman
    SKU:25073 - 5 mg

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  • Filipin II is a polyene and an active component of the polyene antibiotic filipin complex (Item No. 25073).{39829} It has broad-spectrum antifungal activity, reducing growth of various fungi, including B. dermatitidis, C. neoformans, and H. capsulatum (MICs = 1-10 μg/ml). Filipin II inhibits ADP-stimulated respiration in rat liver mitochondria when used at a concentration of 3.5 mg/ml.{39830} It also induces hemolysis of liposomes in a cholesterol-independent manner (IC50 = 0.5 μg/ml).{39831}  

     

    Brand:
    Cayman
    SKU:25521 - 2.5 mg

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  • Filipin II is a polyene and an active component of the polyene antibiotic filipin complex (Item No. 25073).{39829} It has broad-spectrum antifungal activity, reducing growth of various fungi, including B. dermatitidis, C. neoformans, and H. capsulatum (MICs = 1-10 μg/ml). Filipin II inhibits ADP-stimulated respiration in rat liver mitochondria when used at a concentration of 3.5 mg/ml.{39830} It also induces hemolysis of liposomes in a cholesterol-independent manner (IC50 = 0.5 μg/ml).{39831}  

     

    Brand:
    Cayman
    SKU:25521 - 500 µg

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  • Cholesterol is both an important structural component of cell membranes and an early intermediate in hormone and bile acid biosynthesis. The localization and measurement of cholesterol in cells is therefore of great interest. Filipin is the collective name given to four isomeric polyene macrolides isolated from cultures of S. filipinensis; Filipin III is the predominant isomer and the one used in most studies. Filipin binds to cholesterol in membranes, forming ultrastructural aggregates and complexes which can be visualized by freeze-fracture electron microscopy.{8625,9103} The binding of cholesterol also decreases the intrinsic fluorescence of Filipin, and this property has also been used to detect cholesterol in membrane fractions.{9104}  

     

    Brand:
    Cayman
    SKU:70440 - 1 mg

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  • Cholesterol is both an important structural component of cell membranes and an early intermediate in hormone and bile acid biosynthesis. The localization and measurement of cholesterol in cells is therefore of great interest. Filipin is the collective name given to four isomeric polyene macrolides isolated from cultures of S. filipinensis; Filipin III is the predominant isomer and the one used in most studies. Filipin binds to cholesterol in membranes, forming ultrastructural aggregates and complexes which can be visualized by freeze-fracture electron microscopy.{8625,9103} The binding of cholesterol also decreases the intrinsic fluorescence of Filipin, and this property has also been used to detect cholesterol in membrane fractions.{9104}  

     

    Brand:
    Cayman
    SKU:70440 - 5 mg

    Available on backorder

  • Cholesterol is both an important structural component of cell membranes and an early intermediate in hormone and bile acid biosynthesis. The localization and measurement of cholesterol in cells is therefore of great interest. Filipin is the collective name given to four isomeric polyene macrolides isolated from cultures of S. filipinensis; Filipin III is the predominant isomer and the one used in most studies. Filipin binds to cholesterol in membranes, forming ultrastructural aggregates and complexes which can be visualized by freeze-fracture electron microscopy.{8625,9103} The binding of cholesterol also decreases the intrinsic fluorescence of Filipin, and this property has also been used to detect cholesterol in membrane fractions.{9104}  

     

    Brand:
    Cayman
    SKU:70440 - 500 µg

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  • Filorexant is a dual antagonist of orexin 1 receptor (OX1R) and OX2R (Kis = 2.5 and 0.31 nM, respectively, for the recombinant human receptors).{48849} It selectively inhibits OX1R and OX2R over a panel of more than 170 receptors and enzymes. Filorexant inhibits orexin A-induced calcium mobilization in CHO cells expressing recombinant human OX1R or OX2R (Kb = 11 nM for both). It decreases locomotor activity in rats during the dark cycle when administered at a dose of 10 mg/kg. Filorexant (0.5 mg/kg) reduces the time spent awake and decreases the latency to slow-wave sleep stage 1 (SWS1) and SWS2, but not rapid eye movement (REM) sleep, in dogs. It increases the duration of SWS2, but not SWS1 or REM sleep, in the same model.  

     

    Brand:
    Cayman
    SKU:29490 - 10 mg

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  • Filorexant is a dual antagonist of orexin 1 receptor (OX1R) and OX2R (Kis = 2.5 and 0.31 nM, respectively, for the recombinant human receptors).{48849} It selectively inhibits OX1R and OX2R over a panel of more than 170 receptors and enzymes. Filorexant inhibits orexin A-induced calcium mobilization in CHO cells expressing recombinant human OX1R or OX2R (Kb = 11 nM for both). It decreases locomotor activity in rats during the dark cycle when administered at a dose of 10 mg/kg. Filorexant (0.5 mg/kg) reduces the time spent awake and decreases the latency to slow-wave sleep stage 1 (SWS1) and SWS2, but not rapid eye movement (REM) sleep, in dogs. It increases the duration of SWS2, but not SWS1 or REM sleep, in the same model.  

     

    Brand:
    Cayman
    SKU:29490 - 25 mg

    Available on backorder

  • Filorexant is a dual antagonist of orexin 1 receptor (OX1R) and OX2R (Kis = 2.5 and 0.31 nM, respectively, for the recombinant human receptors).{48849} It selectively inhibits OX1R and OX2R over a panel of more than 170 receptors and enzymes. Filorexant inhibits orexin A-induced calcium mobilization in CHO cells expressing recombinant human OX1R or OX2R (Kb = 11 nM for both). It decreases locomotor activity in rats during the dark cycle when administered at a dose of 10 mg/kg. Filorexant (0.5 mg/kg) reduces the time spent awake and decreases the latency to slow-wave sleep stage 1 (SWS1) and SWS2, but not rapid eye movement (REM) sleep, in dogs. It increases the duration of SWS2, but not SWS1 or REM sleep, in the same model.  

     

    Brand:
    Cayman
    SKU:29490 - 5 mg

    Available on backorder

  • Filorexant is a dual antagonist of orexin 1 receptor (OX1R) and OX2R (Kis = 2.5 and 0.31 nM, respectively, for the recombinant human receptors).{48849} It selectively inhibits OX1R and OX2R over a panel of more than 170 receptors and enzymes. Filorexant inhibits orexin A-induced calcium mobilization in CHO cells expressing recombinant human OX1R or OX2R (Kb = 11 nM for both). It decreases locomotor activity in rats during the dark cycle when administered at a dose of 10 mg/kg. Filorexant (0.5 mg/kg) reduces the time spent awake and decreases the latency to slow-wave sleep stage 1 (SWS1) and SWS2, but not rapid eye movement (REM) sleep, in dogs. It increases the duration of SWS2, but not SWS1 or REM sleep, in the same model.  

     

    Brand:
    Cayman
    SKU:29490 - 50 mg

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  • FIN56 is an inducer of ferroptosis and a derivative of CIL56 (Item No. 19287).{39186} It selectively induces ferroptosis in BJ cells overexpressing oncogenic HRASG12V via acetyl-CoA carboxylase-dependent reduction in expression of GPX4 protein. This effect is reversed by the ferroptosis inhibitors deferoxamine (Item No. 14595) and α-tocopherol as well as overexpression of the fusion protein GFP-GPX4. FIN56 also binds to and activates squalene synthase in a GPX4 degradation-independent manner.  

     

    Brand:
    Cayman
    SKU:25180 - 10 mg

    Available on backorder

  • FIN56 is an inducer of ferroptosis and a derivative of CIL56 (Item No. 19287).{39186} It selectively induces ferroptosis in BJ cells overexpressing oncogenic HRASG12V via acetyl-CoA carboxylase-dependent reduction in expression of GPX4 protein. This effect is reversed by the ferroptosis inhibitors deferoxamine (Item No. 14595) and α-tocopherol as well as overexpression of the fusion protein GFP-GPX4. FIN56 also binds to and activates squalene synthase in a GPX4 degradation-independent manner.  

     

    Brand:
    Cayman
    SKU:25180 - 25 mg

    Available on backorder

  • FIN56 is an inducer of ferroptosis and a derivative of CIL56 (Item No. 19287).{39186} It selectively induces ferroptosis in BJ cells overexpressing oncogenic HRASG12V via acetyl-CoA carboxylase-dependent reduction in expression of GPX4 protein. This effect is reversed by the ferroptosis inhibitors deferoxamine (Item No. 14595) and α-tocopherol as well as overexpression of the fusion protein GFP-GPX4. FIN56 also binds to and activates squalene synthase in a GPX4 degradation-independent manner.  

     

    Brand:
    Cayman
    SKU:25180 - 5 mg

    Available on backorder

  • FIN56 is an inducer of ferroptosis and a derivative of CIL56 (Item No. 19287).{39186} It selectively induces ferroptosis in BJ cells overexpressing oncogenic HRASG12V via acetyl-CoA carboxylase-dependent reduction in expression of GPX4 protein. This effect is reversed by the ferroptosis inhibitors deferoxamine (Item No. 14595) and α-tocopherol as well as overexpression of the fusion protein GFP-GPX4. FIN56 also binds to and activates squalene synthase in a GPX4 degradation-independent manner.  

     

    Brand:
    Cayman
    SKU:25180 - 50 mg

    Available on backorder

  • Brand:
    Cayman
    SKU:22410 -

    Out of stock

  • Brand:
    Cayman
    SKU:22410 -

    Out of stock

  • Brand:
    Cayman
    SKU:22410 -

    Out of stock

  • Finasteride is a 4-azasteroid competitive inhibitor of 5α-reductase type II (IC50 = 4.2 nM) and a derivative of testosterone.{23862} It is 100-fold selective for 5α-reductase type II over type I. Finasteride (10 µM) does not affect the growth of androgen-refractory PC3 prostate cancer cells but increases the protein levels of Nrf2 and heme oxygenase-1 (HO-1).{23866} It decreases prostatic diameter and volume, as well as dihydrotestosterone, but not testosterone, serum levels in dogs with spontaneous benign prostatic hypertrophy when administered at doses of 0.1 and 0.5 mg/kg.{48477} Finasteride reduces testosterone-induced type I procollagen and TGF-β1 protein levels in cultured human scalp dermal fibroblasts in a model of androgenic alopecia when applied at a concentration of 0.1 μM.{23865} Formulations containing finasteride have been used in the treatment of benign prostatic hyperplasia and androgenic alopecia in men.  

     

    Brand:
    Cayman
    SKU:-
  • Finasteride is a 4-azasteroid competitive inhibitor of 5α-reductase type II (IC50 = 4.2 nM) and a derivative of testosterone.{23862} It is 100-fold selective for 5α-reductase type II over type I. Finasteride (10 µM) does not affect the growth of androgen-refractory PC3 prostate cancer cells but increases the protein levels of Nrf2 and heme oxygenase-1 (HO-1).{23866} It decreases prostatic diameter and volume, as well as dihydrotestosterone, but not testosterone, serum levels in dogs with spontaneous benign prostatic hypertrophy when administered at doses of 0.1 and 0.5 mg/kg.{48477} Finasteride reduces testosterone-induced type I procollagen and TGF-β1 protein levels in cultured human scalp dermal fibroblasts in a model of androgenic alopecia when applied at a concentration of 0.1 μM.{23865} Formulations containing finasteride have been used in the treatment of benign prostatic hyperplasia and androgenic alopecia in men.  

     

    Brand:
    Cayman
    SKU:-
  • Finasteride is a 4-azasteroid competitive inhibitor of 5α-reductase type II (IC50 = 4.2 nM) and a derivative of testosterone.{23862} It is 100-fold selective for 5α-reductase type II over type I. Finasteride (10 µM) does not affect the growth of androgen-refractory PC3 prostate cancer cells but increases the protein levels of Nrf2 and heme oxygenase-1 (HO-1).{23866} It decreases prostatic diameter and volume, as well as dihydrotestosterone, but not testosterone, serum levels in dogs with spontaneous benign prostatic hypertrophy when administered at doses of 0.1 and 0.5 mg/kg.{48477} Finasteride reduces testosterone-induced type I procollagen and TGF-β1 protein levels in cultured human scalp dermal fibroblasts in a model of androgenic alopecia when applied at a concentration of 0.1 μM.{23865} Formulations containing finasteride have been used in the treatment of benign prostatic hyperplasia and androgenic alopecia in men.  

     

    Brand:
    Cayman
    SKU:-
  • Finasteride-d9 is intended for use as an internal standard for the quantification of finasteride (Item No. 14938) by GC- or LC-MS. Finasteride is a 4-azasteroid competitive inhibitor of 5α-reductase type II (IC50 = 4.2 nM) and a derivative of testosterone.{23862} It is 100-fold selective for 5α-reductase type II over type I. Finasteride (10 µM) does not affect the growth of androgen-refractory PC3 prostate cancer cells but increases the protein levels of Nrf2 and heme oxygenase-1 (HO-1).{23866} It decreases prostatic diameter and volume, as well as dihydrotestosterone, but not testosterone, serum levels in dogs with spontaneous benign prostatic hypertrophy when administered at doses of 0.1 and 0.5 mg/kg.{48477} Finasteride reduces testosterone-induced type I procollagen and TGF-β1 protein levels in cultured human scalp dermal fibroblasts in a model of androgenic alopecia when applied at a concentration of 0.1 μM.{23865} Formulations containing finasteride have been used in the treatment of benign prostatic hyperplasia and androgenic alopecia in men.  

     

    Brand:
    Cayman
    SKU:28482 - 1 mg

    Available on backorder

  • Finasteride-d9 is intended for use as an internal standard for the quantification of finasteride (Item No. 14938) by GC- or LC-MS. Finasteride is a 4-azasteroid competitive inhibitor of 5α-reductase type II (IC50 = 4.2 nM) and a derivative of testosterone.{23862} It is 100-fold selective for 5α-reductase type II over type I. Finasteride (10 µM) does not affect the growth of androgen-refractory PC3 prostate cancer cells but increases the protein levels of Nrf2 and heme oxygenase-1 (HO-1).{23866} It decreases prostatic diameter and volume, as well as dihydrotestosterone, but not testosterone, serum levels in dogs with spontaneous benign prostatic hypertrophy when administered at doses of 0.1 and 0.5 mg/kg.{48477} Finasteride reduces testosterone-induced type I procollagen and TGF-β1 protein levels in cultured human scalp dermal fibroblasts in a model of androgenic alopecia when applied at a concentration of 0.1 μM.{23865} Formulations containing finasteride have been used in the treatment of benign prostatic hyperplasia and androgenic alopecia in men.  

     

    Brand:
    Cayman
    SKU:28482 - 500 µg

    Available on backorder

  • Fingolimod is a derivative of ISP-1 (myriocin), a fungal metabolite of the Chinese herb I. sinclarii as well as a structural analog of sphingosine. It is a novel immune modulator that prolongs allograft transplant survival in numerous models by inhibiting lymphocyte emigration from lymphoid organs.{11265} Fingolimod is phosphorylated by sphingosine kinase, which then acts as a potent agonist at four of the sphingosine-1-phosphate (S1P) receptors (S1P1, S1P3, S1P4, and S1P5).{11284} Down-regulation of S1P1 receptors on T and B lymphocytes by fingolimod results in defective egress of these cells from spleen, lymph nodes, and Peyer’s patch.{11738} Fingolimod also enhances the activity of the sphingosine transporter Abcb1 and the leukotriene C4 transporter Abcc1 and inhibits cytosolic phospholipase A2 (PLA2) activity.{11283,14604}  

     

    Brand:
    Cayman
    SKU:11975 - 10 mg

    Available on backorder

  • Fingolimod is a derivative of ISP-1 (myriocin), a fungal metabolite of the Chinese herb I. sinclarii as well as a structural analog of sphingosine. It is a novel immune modulator that prolongs allograft transplant survival in numerous models by inhibiting lymphocyte emigration from lymphoid organs.{11265} Fingolimod is phosphorylated by sphingosine kinase, which then acts as a potent agonist at four of the sphingosine-1-phosphate (S1P) receptors (S1P1, S1P3, S1P4, and S1P5).{11284} Down-regulation of S1P1 receptors on T and B lymphocytes by fingolimod results in defective egress of these cells from spleen, lymph nodes, and Peyer’s patch.{11738} Fingolimod also enhances the activity of the sphingosine transporter Abcb1 and the leukotriene C4 transporter Abcc1 and inhibits cytosolic phospholipase A2 (PLA2) activity.{11283,14604}  

     

    Brand:
    Cayman
    SKU:11975 - 25 mg

    Available on backorder

  • Fingolimod is a derivative of ISP-1 (myriocin), a fungal metabolite of the Chinese herb I. sinclarii as well as a structural analog of sphingosine. It is a novel immune modulator that prolongs allograft transplant survival in numerous models by inhibiting lymphocyte emigration from lymphoid organs.{11265} Fingolimod is phosphorylated by sphingosine kinase, which then acts as a potent agonist at four of the sphingosine-1-phosphate (S1P) receptors (S1P1, S1P3, S1P4, and S1P5).{11284} Down-regulation of S1P1 receptors on T and B lymphocytes by fingolimod results in defective egress of these cells from spleen, lymph nodes, and Peyer’s patch.{11738} Fingolimod also enhances the activity of the sphingosine transporter Abcb1 and the leukotriene C4 transporter Abcc1 and inhibits cytosolic phospholipase A2 (PLA2) activity.{11283,14604}  

     

    Brand:
    Cayman
    SKU:11975 - 5 mg

    Available on backorder

  • Fingolimod is a derivative of ISP-1 (myriocin), a fungal metabolite of the Chinese herb I. sinclarii as well as a structural analog of sphingosine. It is a novel immune modulator that prolongs allograft transplant survival in numerous models by inhibiting lymphocyte emigration from lymphoid organs.{11265} Fingolimod is phosphorylated by sphingosine kinase, which then acts as a potent agonist at four of the sphingosine-1-phosphate (S1P) receptors (S1P1, S1P3, S1P4, and S1P5).{11284} Down-regulation of S1P1 receptors on T and B lymphocytes by fingolimod results in defective egress of these cells from spleen, lymph nodes, and Peyer’s patch.{11738} Fingolimod also enhances the activity of the sphingosine transporter Abcb1 and the leukotriene C4 transporter Abcc1 and inhibits cytosolic phospholipase A2 (PLA2) activity.{11283,14604}  

     

    Brand:
    Cayman
    SKU:11975 - 50 mg

    Available on backorder

  • Fingolimod is a derivative of ISP-1 (myriocin), a fungal metabolite of the Chinese herb Iscaria sinclarii as well as a structural analog of sphingosine. It is a novel immune modulator that prolongs allograft transplant survival in numerous models by inhibiting lymphocyte emigration from lymphoid organs.{11265} Fingolimod is phosphorylated by sphingosine kinase, which then acts as a potent agonist at four of the sphingosine-1-phosphate (S1P) receptors (S1P1, S1P3, S1P4, and S1P5).{11284} Down-regulation of S1P1 receptors on T and B lymphocytes by fingolimod results in defective egress of these cells from spleen, lymph nodes, and Peyer’s patch.{11738} Fingolimod also enhances the activity of the sphingosine transporter Abcb1 and the leukotriene C4 transporter Abcc1 and inhibits cytosolic phospholipase A2 activity.{11283,14604}  

     

    Brand:
    Cayman
    SKU:10006292 - 1 g

    Available on backorder

  • Fingolimod is a derivative of ISP-1 (myriocin), a fungal metabolite of the Chinese herb Iscaria sinclarii as well as a structural analog of sphingosine. It is a novel immune modulator that prolongs allograft transplant survival in numerous models by inhibiting lymphocyte emigration from lymphoid organs.{11265} Fingolimod is phosphorylated by sphingosine kinase, which then acts as a potent agonist at four of the sphingosine-1-phosphate (S1P) receptors (S1P1, S1P3, S1P4, and S1P5).{11284} Down-regulation of S1P1 receptors on T and B lymphocytes by fingolimod results in defective egress of these cells from spleen, lymph nodes, and Peyer’s patch.{11738} Fingolimod also enhances the activity of the sphingosine transporter Abcb1 and the leukotriene C4 transporter Abcc1 and inhibits cytosolic phospholipase A2 activity.{11283,14604}  

     

    Brand:
    Cayman
    SKU:10006292 - 100 mg

    Available on backorder

  • Fingolimod is a derivative of ISP-1 (myriocin), a fungal metabolite of the Chinese herb Iscaria sinclarii as well as a structural analog of sphingosine. It is a novel immune modulator that prolongs allograft transplant survival in numerous models by inhibiting lymphocyte emigration from lymphoid organs.{11265} Fingolimod is phosphorylated by sphingosine kinase, which then acts as a potent agonist at four of the sphingosine-1-phosphate (S1P) receptors (S1P1, S1P3, S1P4, and S1P5).{11284} Down-regulation of S1P1 receptors on T and B lymphocytes by fingolimod results in defective egress of these cells from spleen, lymph nodes, and Peyer’s patch.{11738} Fingolimod also enhances the activity of the sphingosine transporter Abcb1 and the leukotriene C4 transporter Abcc1 and inhibits cytosolic phospholipase A2 activity.{11283,14604}  

     

    Brand:
    Cayman
    SKU:10006292 - 250 mg

    Available on backorder

  • Fingolimod is a derivative of ISP-1 (myriocin), a fungal metabolite of the Chinese herb Iscaria sinclarii as well as a structural analog of sphingosine. It is a novel immune modulator that prolongs allograft transplant survival in numerous models by inhibiting lymphocyte emigration from lymphoid organs.{11265} Fingolimod is phosphorylated by sphingosine kinase, which then acts as a potent agonist at four of the sphingosine-1-phosphate (S1P) receptors (S1P1, S1P3, S1P4, and S1P5).{11284} Down-regulation of S1P1 receptors on T and B lymphocytes by fingolimod results in defective egress of these cells from spleen, lymph nodes, and Peyer’s patch.{11738} Fingolimod also enhances the activity of the sphingosine transporter Abcb1 and the leukotriene C4 transporter Abcc1 and inhibits cytosolic phospholipase A2 activity.{11283,14604}  

     

    Brand:
    Cayman
    SKU:10006292 - 50 mg

    Available on backorder

  • Fingolimod-d4 is intended for use as an internal standard for the quantification of fingolimod (Item Nos. 11975 | 10006292) by GC- or LC-MS. Fingolimod is a derivative of ISP-1 (myriocin), a fungal metabolite of the Chinese herb I. sinclarii as well as a structural analog of sphingosine. It is a novel immune modulator that prolongs allograft transplant survival in numerous models by inhibiting lymphocyte emigration from lymphoid organs.{11265} Fingolimod is phosphorylated by sphingosine kinase, which then acts as a potent agonist at four of the sphingosine-1-phosphate (S1P) receptors (S1P1, S1P3, S1P4, and S1P5).{11284} Down-regulation of S1P1 receptors on T and B lymphocytes by fingolimod results in defective egress of these cells from spleen, lymph nodes, and Peyer’s patch.{11738} Fingolimod also enhances the activity of the sphingosine transporter Abcb1 and the leukotriene C4 transporter Abcc1 and inhibits cytosolic phospholipase A2 activity.{11283,14604}  

     

    Brand:
    Cayman
    SKU:25037 - 1 mg

    Available on backorder

  • Fingolimod-d4 is intended for use as an internal standard for the quantification of fingolimod (Item Nos. 11975 | 10006292) by GC- or LC-MS. Fingolimod is a derivative of ISP-1 (myriocin), a fungal metabolite of the Chinese herb I. sinclarii as well as a structural analog of sphingosine. It is a novel immune modulator that prolongs allograft transplant survival in numerous models by inhibiting lymphocyte emigration from lymphoid organs.{11265} Fingolimod is phosphorylated by sphingosine kinase, which then acts as a potent agonist at four of the sphingosine-1-phosphate (S1P) receptors (S1P1, S1P3, S1P4, and S1P5).{11284} Down-regulation of S1P1 receptors on T and B lymphocytes by fingolimod results in defective egress of these cells from spleen, lymph nodes, and Peyer’s patch.{11738} Fingolimod also enhances the activity of the sphingosine transporter Abcb1 and the leukotriene C4 transporter Abcc1 and inhibits cytosolic phospholipase A2 activity.{11283,14604}  

     

    Brand:
    Cayman
    SKU:25037 - 500 µg

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  • FINO2 is a ferroptosis-inducing peroxide compound that indirectly inhibits glutathione peroxidase 4 (GPX4) and oxidizes iron.{35318} It decreases GPX4 activity and protein levels in vitro but does not act as an active site, allosteric, or covalent inhibitor of GPX4 or alter GPX homeostasis. It also oxidizes iron in vitro, leading to degradation of the endoperoxide moiety, but does not affect the protein levels of iron regulatory proteins, such as IRP2, FTL1, or TFR. FINO2 induces lipid peroxidation of a large subset of the lipidome in HT-1080 cells when used at a concentration of 10 µM and induces ferroptosis in an arachidonic acid lipoxygenase-independent manner. It inhibits cell growth (mean GI50 = 5.8 µM) and induces lethality (mean LC50 = 46 µM) in the NCI-60 panel of cancer cell lines.{35102} It is selective for oncogenically transformed BJ-ELR cells over noncancerous BJ-hTERT cells when used at concentrations of 15 and 20 µM. FINO2 (6 µM) induces oxidative stress, including lipid peroxidation, in RS4;11 B-lymphoblastic leukemia cells. It induces iron-dependent cell death, an effect that can be blocked by pretreatment with the lipophilic antioxidants ferrostatin-1 (Item No. 17729) and liproxstatin-1 (Item No. 17730), and does not induce markers of apoptosis, necrosis, or autophagy in RS4;11 cells.  

     

    Brand:
    Cayman
    SKU:25096 - 1 mg

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  • FINO2 is a ferroptosis-inducing peroxide compound that indirectly inhibits glutathione peroxidase 4 (GPX4) and oxidizes iron.{35318} It decreases GPX4 activity and protein levels in vitro but does not act as an active site, allosteric, or covalent inhibitor of GPX4 or alter GPX homeostasis. It also oxidizes iron in vitro, leading to degradation of the endoperoxide moiety, but does not affect the protein levels of iron regulatory proteins, such as IRP2, FTL1, or TFR. FINO2 induces lipid peroxidation of a large subset of the lipidome in HT-1080 cells when used at a concentration of 10 µM and induces ferroptosis in an arachidonic acid lipoxygenase-independent manner. It inhibits cell growth (mean GI50 = 5.8 µM) and induces lethality (mean LC50 = 46 µM) in the NCI-60 panel of cancer cell lines.{35102} It is selective for oncogenically transformed BJ-ELR cells over noncancerous BJ-hTERT cells when used at concentrations of 15 and 20 µM. FINO2 (6 µM) induces oxidative stress, including lipid peroxidation, in RS4;11 B-lymphoblastic leukemia cells. It induces iron-dependent cell death, an effect that can be blocked by pretreatment with the lipophilic antioxidants ferrostatin-1 (Item No. 17729) and liproxstatin-1 (Item No. 17730), and does not induce markers of apoptosis, necrosis, or autophagy in RS4;11 cells.  

     

    Brand:
    Cayman
    SKU:25096 - 10 mg

    Available on backorder

  • FINO2 is a ferroptosis-inducing peroxide compound that indirectly inhibits glutathione peroxidase 4 (GPX4) and oxidizes iron.{35318} It decreases GPX4 activity and protein levels in vitro but does not act as an active site, allosteric, or covalent inhibitor of GPX4 or alter GPX homeostasis. It also oxidizes iron in vitro, leading to degradation of the endoperoxide moiety, but does not affect the protein levels of iron regulatory proteins, such as IRP2, FTL1, or TFR. FINO2 induces lipid peroxidation of a large subset of the lipidome in HT-1080 cells when used at a concentration of 10 µM and induces ferroptosis in an arachidonic acid lipoxygenase-independent manner. It inhibits cell growth (mean GI50 = 5.8 µM) and induces lethality (mean LC50 = 46 µM) in the NCI-60 panel of cancer cell lines.{35102} It is selective for oncogenically transformed BJ-ELR cells over noncancerous BJ-hTERT cells when used at concentrations of 15 and 20 µM. FINO2 (6 µM) induces oxidative stress, including lipid peroxidation, in RS4;11 B-lymphoblastic leukemia cells. It induces iron-dependent cell death, an effect that can be blocked by pretreatment with the lipophilic antioxidants ferrostatin-1 (Item No. 17729) and liproxstatin-1 (Item No. 17730), and does not induce markers of apoptosis, necrosis, or autophagy in RS4;11 cells.  

     

    Brand:
    Cayman
    SKU:25096 - 5 mg

    Available on backorder

  • FINO2 is a ferroptosis-inducing peroxide compound that indirectly inhibits glutathione peroxidase 4 (GPX4) and oxidizes iron.{35318} It decreases GPX4 activity and protein levels in vitro but does not act as an active site, allosteric, or covalent inhibitor of GPX4 or alter GPX homeostasis. It also oxidizes iron in vitro, leading to degradation of the endoperoxide moiety, but does not affect the protein levels of iron regulatory proteins, such as IRP2, FTL1, or TFR. FINO2 induces lipid peroxidation of a large subset of the lipidome in HT-1080 cells when used at a concentration of 10 µM and induces ferroptosis in an arachidonic acid lipoxygenase-independent manner. It inhibits cell growth (mean GI50 = 5.8 µM) and induces lethality (mean LC50 = 46 µM) in the NCI-60 panel of cancer cell lines.{35102} It is selective for oncogenically transformed BJ-ELR cells over noncancerous BJ-hTERT cells when used at concentrations of 15 and 20 µM. FINO2 (6 µM) induces oxidative stress, including lipid peroxidation, in RS4;11 B-lymphoblastic leukemia cells. It induces iron-dependent cell death, an effect that can be blocked by pretreatment with the lipophilic antioxidants ferrostatin-1 (Item No. 17729) and liproxstatin-1 (Item No. 17730), and does not induce markers of apoptosis, necrosis, or autophagy in RS4;11 cells.  

     

    Brand:
    Cayman
    SKU:25096 - 50 mg

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  • Isoforms of phospholipase D (PLD) cleave the head group from phospholipids, releasing the second messenger phosphatidic acid (PA), which can produce changes in Ras activation, cell spreading, stress fiber formation, chemotaxis, and membrane vesicle trafficking. FIPI is a derivative of halopemide which potently inhibits both PLD1 (IC50 = 25 nM) and PLD2 (IC50 = 20 nM).{17399,17462} It also prevents PLD regulation of F-actin cytoskeleton reorganization, cell spreading, and chemotaxis.{17399} FIPI has good pharmacokinetic parameters in rats, with a half-life greater than five hours, a Cmax that, at 363 nM, is greater than 10-fold the IC50 versus PLD2, and bioavailability of 18%.{17462}  

     

    Brand:
    Cayman
    SKU:-
  • Isoforms of phospholipase D (PLD) cleave the head group from phospholipids, releasing the second messenger phosphatidic acid (PA), which can produce changes in Ras activation, cell spreading, stress fiber formation, chemotaxis, and membrane vesicle trafficking. FIPI is a derivative of halopemide which potently inhibits both PLD1 (IC50 = 25 nM) and PLD2 (IC50 = 20 nM).{17399,17462} It also prevents PLD regulation of F-actin cytoskeleton reorganization, cell spreading, and chemotaxis.{17399} FIPI has good pharmacokinetic parameters in rats, with a half-life greater than five hours, a Cmax that, at 363 nM, is greater than 10-fold the IC50 versus PLD2, and bioavailability of 18%.{17462}  

     

    Brand:
    Cayman
    SKU:-
  • Isoforms of phospholipase D (PLD) cleave the head group from phospholipids, releasing the second messenger phosphatidic acid (PA), which can produce changes in Ras activation, cell spreading, stress fiber formation, chemotaxis, and membrane vesicle trafficking. FIPI is a derivative of halopemide which potently inhibits both PLD1 (IC50 = 25 nM) and PLD2 (IC50 = 20 nM).{17399,17462} It also prevents PLD regulation of F-actin cytoskeleton reorganization, cell spreading, and chemotaxis.{17399} FIPI has good pharmacokinetic parameters in rats, with a half-life greater than five hours, a Cmax that, at 363 nM, is greater than 10-fold the IC50 versus PLD2, and bioavailability of 18%.{17462}  

     

    Brand:
    Cayman
    SKU:-
  • Isoforms of phospholipase D (PLD) cleave the head group from phospholipids, releasing the second messenger phosphatidic acid (PA), which can produce changes in Ras activation, cell spreading, stress fiber formation, chemotaxis, and membrane vesicle trafficking. FIPI is a derivative of halopemide which potently inhibits both PLD1 (IC50 = 25 nM) and PLD2 (IC50 = 20 nM).{17399,17462} It also prevents PLD regulation of F-actin cytoskeleton reorganization, cell spreading, and chemotaxis.{17399} FIPI has good pharmacokinetic parameters in rats, with a half-life greater than five hours, a Cmax that, at 363 nM, is greater than 10-fold the IC50 versus PLD2, and bioavailability of 18%.{17462}  

     

    Brand:
    Cayman
    SKU:-
  • Fipronil is an insecticide that acts as a selective antagonist of insect GABA receptors (IC50s = 30 and 1,600 nM for cockroach and rat receptors, respectively).{41694} It also inhibits desensitizing and non-desensitizing glutamate-induced chloride currents in cockroach neurons (IC50s = 800 and 10 nM, respectively). Fipronil induces activity of the cytochrome P450 (CYP) isoforms CYP1A1/2, CYP2B1/2, and CYP3A1/2 in isolated rat liver microsomes.{41695} Formulations containing fipronil have been used as insecticides in veterinary care.  

     

    Brand:
    Cayman
    SKU:24128 - 100 mg

    Available on backorder

  • Fipronil is an insecticide that acts as a selective antagonist of insect GABA receptors (IC50s = 30 and 1,600 nM for cockroach and rat receptors, respectively).{41694} It also inhibits desensitizing and non-desensitizing glutamate-induced chloride currents in cockroach neurons (IC50s = 800 and 10 nM, respectively). Fipronil induces activity of the cytochrome P450 (CYP) isoforms CYP1A1/2, CYP2B1/2, and CYP3A1/2 in isolated rat liver microsomes.{41695} Formulations containing fipronil have been used as insecticides in veterinary care.  

     

    Brand:
    Cayman
    SKU:24128 - 50 mg

    Available on backorder

  • Firocoxib is a selective inhibitor of COX-2 (IC50s = 0.13 and 7.5 µM for COX-2 and COX-1, respectively, in isolated cat blood).{50228} It inhibits LPS-induced production of prostaglandin E2 (PGE2; Item No. 14010) in isolated dog, horse, and cat whole blood ex vivo.{50230,50231,50228} Firocoxib decreases lameness, induces analgesia, and improves range of motion in dogs and horses with osteoarthritis when administered at doses of 5 and 0.1 mg/kg per day, respectively.{50232,50233} Formulations containing firocoxib have been used in dogs and horses with osteoarthritis.  

     

    Brand:
    Cayman
    SKU:28286 - 10 mg

    Available on backorder

  • Firocoxib is a selective inhibitor of COX-2 (IC50s = 0.13 and 7.5 µM for COX-2 and COX-1, respectively, in isolated cat blood).{50228} It inhibits LPS-induced production of prostaglandin E2 (PGE2; Item No. 14010) in isolated dog, horse, and cat whole blood ex vivo.{50230,50231,50228} Firocoxib decreases lameness, induces analgesia, and improves range of motion in dogs and horses with osteoarthritis when administered at doses of 5 and 0.1 mg/kg per day, respectively.{50232,50233} Formulations containing firocoxib have been used in dogs and horses with osteoarthritis.  

     

    Brand:
    Cayman
    SKU:28286 - 100 mg

    Available on backorder

  • Firocoxib is a selective inhibitor of COX-2 (IC50s = 0.13 and 7.5 µM for COX-2 and COX-1, respectively, in isolated cat blood).{50228} It inhibits LPS-induced production of prostaglandin E2 (PGE2; Item No. 14010) in isolated dog, horse, and cat whole blood ex vivo.{50230,50231,50228} Firocoxib decreases lameness, induces analgesia, and improves range of motion in dogs and horses with osteoarthritis when administered at doses of 5 and 0.1 mg/kg per day, respectively.{50232,50233} Formulations containing firocoxib have been used in dogs and horses with osteoarthritis.  

     

    Brand:
    Cayman
    SKU:28286 - 50 mg

    Available on backorder

  • Fisetin is a natural flavonol that is structurally and functionally related to kaempferol (Item No. 11852), myricetin (Item No. 10012600), and quercetin (Item No. 10005169). All are potent antioxidants and have anti-inflammatory actions with possible relevance to cancer.{13784,27237,25057} Fisetin and other flavonols act as activators of sirtuin 1, inhibitors of the spleen tyrosine kinase SYK, and suppressors of CD36 gene expression.{20124,24052,16736}  

     

    Brand:
    Cayman
    SKU:-
  • Fisetin is a natural flavonol that is structurally and functionally related to kaempferol (Item No. 11852), myricetin (Item No. 10012600), and quercetin (Item No. 10005169). All are potent antioxidants and have anti-inflammatory actions with possible relevance to cancer.{13784,27237,25057} Fisetin and other flavonols act as activators of sirtuin 1, inhibitors of the spleen tyrosine kinase SYK, and suppressors of CD36 gene expression.{20124,24052,16736}  

     

    Brand:
    Cayman
    SKU:-
  • Fisetin is a natural flavonol that is structurally and functionally related to kaempferol (Item No. 11852), myricetin (Item No. 10012600), and quercetin (Item No. 10005169). All are potent antioxidants and have anti-inflammatory actions with possible relevance to cancer.{13784,27237,25057} Fisetin and other flavonols act as activators of sirtuin 1, inhibitors of the spleen tyrosine kinase SYK, and suppressors of CD36 gene expression.{20124,24052,16736}  

     

    Brand:
    Cayman
    SKU:-
  • FITM is an antagonist of metabotropic glutamate receptor 1 (mGluR1; IC50 = 5.1 nM for the human receptor).{46556} It is selective for mGluR1 over mGluR2, mGluR5, and mGluR8 (IC50s = >10, 7, and >10 µM, respectively). FITM (0.3 mg/kg) decreases methamphetamine-induced hyperlocomotion in mice and reverses disruptions in prepulse inhibition induced by methamphetamine and ketamine in rats when administered at a dose of 1 mg/kg.  

     

    Brand:
    Cayman
    SKU:29219 - 1 mg

    Available on backorder

  • FITM is an antagonist of metabotropic glutamate receptor 1 (mGluR1; IC50 = 5.1 nM for the human receptor).{46556} It is selective for mGluR1 over mGluR2, mGluR5, and mGluR8 (IC50s = >10, 7, and >10 µM, respectively). FITM (0.3 mg/kg) decreases methamphetamine-induced hyperlocomotion in mice and reverses disruptions in prepulse inhibition induced by methamphetamine and ketamine in rats when administered at a dose of 1 mg/kg.  

     

    Brand:
    Cayman
    SKU:29219 - 10 mg

    Available on backorder

  • FITM is an antagonist of metabotropic glutamate receptor 1 (mGluR1; IC50 = 5.1 nM for the human receptor).{46556} It is selective for mGluR1 over mGluR2, mGluR5, and mGluR8 (IC50s = >10, 7, and >10 µM, respectively). FITM (0.3 mg/kg) decreases methamphetamine-induced hyperlocomotion in mice and reverses disruptions in prepulse inhibition induced by methamphetamine and ketamine in rats when administered at a dose of 1 mg/kg.  

     

    Brand:
    Cayman
    SKU:29219 - 25 mg

    Available on backorder

  • FITM is an antagonist of metabotropic glutamate receptor 1 (mGluR1; IC50 = 5.1 nM for the human receptor).{46556} It is selective for mGluR1 over mGluR2, mGluR5, and mGluR8 (IC50s = >10, 7, and >10 µM, respectively). FITM (0.3 mg/kg) decreases methamphetamine-induced hyperlocomotion in mice and reverses disruptions in prepulse inhibition induced by methamphetamine and ketamine in rats when administered at a dose of 1 mg/kg.  

     

    Brand:
    Cayman
    SKU:29219 - 5 mg

    Available on backorder

  • FK3311 is a cell permeable and orally available sulfonanilide that acts as a COX-2 inhibitor and non-steroidal anti-inflammatory drug (NSAID).{39153,39154} FK3311 inhibits LPS-induced thromboxane B2 (TxB2; Item No. 19030) production (IC50 = 316 nM) in vitro and inhibits adjuvant-induced arthritis (ED50 = 0.29 mg/kg) in rats without causing gastrointestinal irritation. FK3311 also alleviates ischemia-repurfusion injury in canine liver and rat lung in vivo.{39155,39156}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • FK3311 is a cell permeable and orally available sulfonanilide that acts as a COX-2 inhibitor and non-steroidal anti-inflammatory drug (NSAID).{39153,39154} FK3311 inhibits LPS-induced thromboxane B2 (TxB2; Item No. 19030) production (IC50 = 316 nM) in vitro and inhibits adjuvant-induced arthritis (ED50 = 0.29 mg/kg) in rats without causing gastrointestinal irritation. FK3311 also alleviates ischemia-repurfusion injury in canine liver and rat lung in vivo.{39155,39156}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • FK3311 is a cell permeable and orally available sulfonanilide that acts as a COX-2 inhibitor and non-steroidal anti-inflammatory drug (NSAID).{39153,39154} FK3311 inhibits LPS-induced thromboxane B2 (TxB2; Item No. 19030) production (IC50 = 316 nM) in vitro and inhibits adjuvant-induced arthritis (ED50 = 0.29 mg/kg) in rats without causing gastrointestinal irritation. FK3311 also alleviates ischemia-repurfusion injury in canine liver and rat lung in vivo.{39155,39156}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • FK3311 is a cell permeable and orally available sulfonanilide that acts as a COX-2 inhibitor and non-steroidal anti-inflammatory drug (NSAID).{39153,39154} FK3311 inhibits LPS-induced thromboxane B2 (TxB2; Item No. 19030) production (IC50 = 316 nM) in vitro and inhibits adjuvant-induced arthritis (ED50 = 0.29 mg/kg) in rats without causing gastrointestinal irritation. FK3311 also alleviates ischemia-repurfusion injury in canine liver and rat lung in vivo.{39155,39156}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • FK-409 is a NO donor. It liberates NO in a time-dependent manner with a half-life of approximately 40 minutes in phosphate buffer (pH 7.4) at 37°C.{4338} The IC50 for the inhibition of platelet aggregation is 4.9 µM.{5421}  

     

    Brand:
    Cayman
    SKU:82290 - 1 mg

    Available on backorder

  • FK-409 is a NO donor. It liberates NO in a time-dependent manner with a half-life of approximately 40 minutes in phosphate buffer (pH 7.4) at 37°C.{4338} The IC50 for the inhibition of platelet aggregation is 4.9 µM.{5421}  

     

    Brand:
    Cayman
    SKU:82290 - 10 mg

    Available on backorder

  • FK-409 is a NO donor. It liberates NO in a time-dependent manner with a half-life of approximately 40 minutes in phosphate buffer (pH 7.4) at 37°C.{4338} The IC50 for the inhibition of platelet aggregation is 4.9 µM.{5421}  

     

    Brand:
    Cayman
    SKU:82290 - 5 mg

    Available on backorder

  • FK-409 is a NO donor. It liberates NO in a time-dependent manner with a half-life of approximately 40 minutes in phosphate buffer (pH 7.4) at 37°C.{4338} The IC50 for the inhibition of platelet aggregation is 4.9 µM.{5421}  

     

    Brand:
    Cayman
    SKU:82290 - 50 mg

    Available on backorder

  • FK-506 is a potent immunosuppressant in the same molecular class as cyclosporin A (Item No. 12088) and rapamycin (Item No. 13346).{5285} Its mechanism of action involves the formation of a high affinity complex (Ki = 0.2 nM) with FK-506 binding protein 12 (FKBP12). This complex then inhibits the activity of the calcium/calmodulin-dependent protein phosphatase, calcineurin, leading to disruption of T cell activation.{13842} The physiological effects of FK-506 also include regulation of nitric oxide neurotoxicity, neurotransmitter release, and regulation of Ca2+ release via the ryanodine and inositol-(1,4,5)-trisphosphate (IP3) receptors.{7042} In the latter case, FKBP12 forms a tight complex with both ryanodine and IP3 receptors which can be disrupted by FK-506, thereby rendering the receptors leaky to Ca2+.  

     

    Brand:
    Cayman
    SKU:10007965 - 10 mg

    Available on backorder

  • FK-506 is a potent immunosuppressant in the same molecular class as cyclosporin A (Item No. 12088) and rapamycin (Item No. 13346).{5285} Its mechanism of action involves the formation of a high affinity complex (Ki = 0.2 nM) with FK-506 binding protein 12 (FKBP12). This complex then inhibits the activity of the calcium/calmodulin-dependent protein phosphatase, calcineurin, leading to disruption of T cell activation.{13842} The physiological effects of FK-506 also include regulation of nitric oxide neurotoxicity, neurotransmitter release, and regulation of Ca2+ release via the ryanodine and inositol-(1,4,5)-trisphosphate (IP3) receptors.{7042} In the latter case, FKBP12 forms a tight complex with both ryanodine and IP3 receptors which can be disrupted by FK-506, thereby rendering the receptors leaky to Ca2+.  

     

    Brand:
    Cayman
    SKU:10007965 - 100 mg

    Available on backorder

  • FK-506 is a potent immunosuppressant in the same molecular class as cyclosporin A (Item No. 12088) and rapamycin (Item No. 13346).{5285} Its mechanism of action involves the formation of a high affinity complex (Ki = 0.2 nM) with FK-506 binding protein 12 (FKBP12). This complex then inhibits the activity of the calcium/calmodulin-dependent protein phosphatase, calcineurin, leading to disruption of T cell activation.{13842} The physiological effects of FK-506 also include regulation of nitric oxide neurotoxicity, neurotransmitter release, and regulation of Ca2+ release via the ryanodine and inositol-(1,4,5)-trisphosphate (IP3) receptors.{7042} In the latter case, FKBP12 forms a tight complex with both ryanodine and IP3 receptors which can be disrupted by FK-506, thereby rendering the receptors leaky to Ca2+.  

     

    Brand:
    Cayman
    SKU:10007965 - 5 mg

    Available on backorder

  • FK-506 is a potent immunosuppressant in the same molecular class as cyclosporin A (Item No. 12088) and rapamycin (Item No. 13346).{5285} Its mechanism of action involves the formation of a high affinity complex (Ki = 0.2 nM) with FK-506 binding protein 12 (FKBP12). This complex then inhibits the activity of the calcium/calmodulin-dependent protein phosphatase, calcineurin, leading to disruption of T cell activation.{13842} The physiological effects of FK-506 also include regulation of nitric oxide neurotoxicity, neurotransmitter release, and regulation of Ca2+ release via the ryanodine and inositol-(1,4,5)-trisphosphate (IP3) receptors.{7042} In the latter case, FKBP12 forms a tight complex with both ryanodine and IP3 receptors which can be disrupted by FK-506, thereby rendering the receptors leaky to Ca2+.  

     

    Brand:
    Cayman
    SKU:10007965 - 50 mg

    Available on backorder

  • FK-506-13C-d2 contains two deuterium atoms located on the carbon-13 bond. It is intended for use as an internal standard for the quantification of FK-506 (Item No. 10007965) by GC- or LC-MS. FK-506 is a potent, clinically-useful immunosuppressant in the same molecular class as cyclosporin A and rapamycin.{5285} Its mechanism of action involves the formation of a high affinity complex (Ki = 0.2 nM) with FK-506 Binding Protein 12 (FKBP12). This complex then inhibits the activity of the calcium/calmodulin-dependent protein phosphatase, calcineurin, leading to disruption of T cell activation.{13842} The physiological effects of FK-506 also include regulation of nitric oxide neurotoxicity, neurotransmitter release, and regulation of Ca2+ release via the ryanodine and inositol-(1,4,5)-trisphosphate (IP3) receptors.{7042} In the latter case, FKBP12 forms a tight complex with both ryanodine and IP3 receptors which can be disrupted by FK-506, thereby rendering the receptors “leaky” to Ca2+.  

     

    Brand:
    Cayman
    SKU:22178 -

    Out of stock

  • FK-866 is a highly specific non-competitive inhibitor of Nampt (Ki = 0.4 nM), causing gradual NAD+ depletion.{17256} In HepG2 human liver carcinoma cells, NAD+ depletion by FK-866 directs delayed cell death by apoptosis (IC50 = ~1 nM).{17256} In normal human smooth muscle cells, FK-866 causes premature senescence, an effect that may be linked to decreased activity of the NAD+-dependent enzyme SIRT1.{17254} Also, FK-866 induces autophagy in SH-SY5Y neuroblastoma cells, as indicated by the formation of LC3-positive vesicles.{17255}  

     

    Brand:
    Cayman
    SKU:-
  • FK-866 is a highly specific non-competitive inhibitor of Nampt (Ki = 0.4 nM), causing gradual NAD+ depletion.{17256} In HepG2 human liver carcinoma cells, NAD+ depletion by FK-866 directs delayed cell death by apoptosis (IC50 = ~1 nM).{17256} In normal human smooth muscle cells, FK-866 causes premature senescence, an effect that may be linked to decreased activity of the NAD+-dependent enzyme SIRT1.{17254} Also, FK-866 induces autophagy in SH-SY5Y neuroblastoma cells, as indicated by the formation of LC3-positive vesicles.{17255}  

     

    Brand:
    Cayman
    SKU:-
  • FK-866 is a highly specific non-competitive inhibitor of Nampt (Ki = 0.4 nM), causing gradual NAD+ depletion.{17256} In HepG2 human liver carcinoma cells, NAD+ depletion by FK-866 directs delayed cell death by apoptosis (IC50 = ~1 nM).{17256} In normal human smooth muscle cells, FK-866 causes premature senescence, an effect that may be linked to decreased activity of the NAD+-dependent enzyme SIRT1.{17254} Also, FK-866 induces autophagy in SH-SY5Y neuroblastoma cells, as indicated by the formation of LC3-positive vesicles.{17255}  

     

    Brand:
    Cayman
    SKU:-
  • FK-866 is a highly specific non-competitive inhibitor of Nampt (Ki = 0.4 nM), causing gradual NAD+ depletion.{17256} In HepG2 human liver carcinoma cells, NAD+ depletion by FK-866 directs delayed cell death by apoptosis (IC50 = ~1 nM).{17256} In normal human smooth muscle cells, FK-866 causes premature senescence, an effect that may be linked to decreased activity of the NAD+-dependent enzyme SIRT1.{17254} Also, FK-866 induces autophagy in SH-SY5Y neuroblastoma cells, as indicated by the formation of LC3-positive vesicles.{17255}  

     

    Brand:
    Cayman
    SKU:-
  • Phospholipase A2 (PLA2) catalyzes the hydrolysis of fatty acids at the sn-2 position of glycerophospholipids, yielding a free fatty acid and a lysophospholipid as products. There are three broad classes of PLA2, secretory (sPLA2), calcium-dependent cytosolic (cPLA2), and calcium-independent cytosolic (iPLA2), that have different functions. FKGK 11 is a selective inhibitor of iPLA2 that demonstrates an XI(50) value of 0.0073, where XI(50) equals the mole fraction of FKGK 11 in the total substrate interface required to inhibit iPLA2 by 50%.{16700} In comparison, mole fractions as high as 0.091 do not inhibit cPLA2 activity and cause only slight inhibition of sPLA2.{16700}  

     

    Brand:
    Cayman
    SKU:-
  • Phospholipase A2 (PLA2) catalyzes the hydrolysis of fatty acids at the sn-2 position of glycerophospholipids, yielding a free fatty acid and a lysophospholipid as products. There are three broad classes of PLA2, secretory (sPLA2), calcium-dependent cytosolic (cPLA2), and calcium-independent cytosolic (iPLA2), that have different functions. FKGK 11 is a selective inhibitor of iPLA2 that demonstrates an XI(50) value of 0.0073, where XI(50) equals the mole fraction of FKGK 11 in the total substrate interface required to inhibit iPLA2 by 50%.{16700} In comparison, mole fractions as high as 0.091 do not inhibit cPLA2 activity and cause only slight inhibition of sPLA2.{16700}  

     

    Brand:
    Cayman
    SKU:-
  • Phospholipase A2 (PLA2) catalyzes the hydrolysis of fatty acids at the sn-2 position of glycerophospholipids, yielding a free fatty acid and a lysophospholipid as products. There are three broad classes of PLA2, secretory (sPLA2), calcium-dependent cytosolic (cPLA2), and calcium-independent cytosolic (iPLA2), that have different functions. FKGK 11 is a selective inhibitor of iPLA2 that demonstrates an XI(50) value of 0.0073, where XI(50) equals the mole fraction of FKGK 11 in the total substrate interface required to inhibit iPLA2 by 50%.{16700} In comparison, mole fractions as high as 0.091 do not inhibit cPLA2 activity and cause only slight inhibition of sPLA2.{16700}  

     

    Brand:
    Cayman
    SKU:-
  • Phospholipase A2 (PLA2) catalyzes the hydrolysis of fatty acids at the sn-2 position of glycerophospholipids, yielding a free fatty acid and a lysophospholipid as products. There are three broad classes of PLA2, secretory (sPLA2), calcium-dependent cytosolic (cPLA2), and calcium-independent cytosolic (iPLA2), that have different functions. FKGK 11 is a selective inhibitor of iPLA2 that demonstrates an XI(50) value of 0.0073, where XI(50) equals the mole fraction of FKGK 11 in the total substrate interface required to inhibit iPLA2 by 50%.{16700} In comparison, mole fractions as high as 0.091 do not inhibit cPLA2 activity and cause only slight inhibition of sPLA2.{16700}  

     

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  • FKGK 18 is an inhibitor of group VIA (GVIA) calcium-independent phospholipase A2 (iPLA2).{21518} It inhibits GVIA iPLA2 by 99.9% at 0.091 mole fraction in a mixed micelle activity assay and is selective for GVIA iPLA2 over GIVA cPLA2 and GV sPLA2 where it shows 80.8 and 36.8% inhibition, respectively. FKGK 18 inhibits iPLA2β activity in cytosolic extracts from INS-1 cells overexpressing iPLA2β (IC50 = ~50 nM) as well as iPLA2γ activity in mouse heart membrane fractions (IC50s = ~1-3 μM).{42790} It inhibits glucose-induced increases in prostaglandin E2 (PGE2; Item No. 14010) production and insulin secretion in human pancreatic islets when used at a concentration of 10 μM and inhibits thapsigargin-induced apoptosis in INS-1 cells overexpressing iPLA2β in a concentration-dependent manner. FKGK 18 (20 mg/kg, 3 times per week) reduces blood glucose levels in an intraperitoneal glucose tolerance test, decreases the incidence of diabetes, and increases serum insulin levels in non-obese diabetic (NOD) mice.{42791}  

     

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    Cayman
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  • FKGK 18 is an inhibitor of group VIA (GVIA) calcium-independent phospholipase A2 (iPLA2).{21518} It inhibits GVIA iPLA2 by 99.9% at 0.091 mole fraction in a mixed micelle activity assay and is selective for GVIA iPLA2 over GIVA cPLA2 and GV sPLA2 where it shows 80.8 and 36.8% inhibition, respectively. FKGK 18 inhibits iPLA2β activity in cytosolic extracts from INS-1 cells overexpressing iPLA2β (IC50 = ~50 nM) as well as iPLA2γ activity in mouse heart membrane fractions (IC50s = ~1-3 μM).{42790} It inhibits glucose-induced increases in prostaglandin E2 (PGE2; Item No. 14010) production and insulin secretion in human pancreatic islets when used at a concentration of 10 μM and inhibits thapsigargin-induced apoptosis in INS-1 cells overexpressing iPLA2β in a concentration-dependent manner. FKGK 18 (20 mg/kg, 3 times per week) reduces blood glucose levels in an intraperitoneal glucose tolerance test, decreases the incidence of diabetes, and increases serum insulin levels in non-obese diabetic (NOD) mice.{42791}  

     

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    Cayman
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  • FKGK 18 is an inhibitor of group VIA (GVIA) calcium-independent phospholipase A2 (iPLA2).{21518} It inhibits GVIA iPLA2 by 99.9% at 0.091 mole fraction in a mixed micelle activity assay and is selective for GVIA iPLA2 over GIVA cPLA2 and GV sPLA2 where it shows 80.8 and 36.8% inhibition, respectively. FKGK 18 inhibits iPLA2β activity in cytosolic extracts from INS-1 cells overexpressing iPLA2β (IC50 = ~50 nM) as well as iPLA2γ activity in mouse heart membrane fractions (IC50s = ~1-3 μM).{42790} It inhibits glucose-induced increases in prostaglandin E2 (PGE2; Item No. 14010) production and insulin secretion in human pancreatic islets when used at a concentration of 10 μM and inhibits thapsigargin-induced apoptosis in INS-1 cells overexpressing iPLA2β in a concentration-dependent manner. FKGK 18 (20 mg/kg, 3 times per week) reduces blood glucose levels in an intraperitoneal glucose tolerance test, decreases the incidence of diabetes, and increases serum insulin levels in non-obese diabetic (NOD) mice.{42791}  

     

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    Cayman
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  • FKGK 18 is an inhibitor of group VIA (GVIA) calcium-independent phospholipase A2 (iPLA2).{21518} It inhibits GVIA iPLA2 by 99.9% at 0.091 mole fraction in a mixed micelle activity assay and is selective for GVIA iPLA2 over GIVA cPLA2 and GV sPLA2 where it shows 80.8 and 36.8% inhibition, respectively. FKGK 18 inhibits iPLA2β activity in cytosolic extracts from INS-1 cells overexpressing iPLA2β (IC50 = ~50 nM) as well as iPLA2γ activity in mouse heart membrane fractions (IC50s = ~1-3 μM).{42790} It inhibits glucose-induced increases in prostaglandin E2 (PGE2; Item No. 14010) production and insulin secretion in human pancreatic islets when used at a concentration of 10 μM and inhibits thapsigargin-induced apoptosis in INS-1 cells overexpressing iPLA2β in a concentration-dependent manner. FKGK 18 (20 mg/kg, 3 times per week) reduces blood glucose levels in an intraperitoneal glucose tolerance test, decreases the incidence of diabetes, and increases serum insulin levels in non-obese diabetic (NOD) mice.{42791}  

     

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  • Flambalactone is a degradation product formed by methanolysis of the antibiotic flambamycin.{36636}  

     

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    Cayman
    SKU:24916 - 1 mg

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  • Flambalactone is a degradation product formed by methanolysis of the antibiotic flambamycin.{36636}  

     

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    Cayman
    SKU:24916 - 5 mg

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  • FlAsH-EDT2 is a pro-fluorescent, membrane-permeable biarsenical compound that binds covalently to a tetracysteine sequence (CCPGCC), which is engineered into target proteins.{33065,31942} It binds proteins that have the CCPGCC tag almost immediately after translation.{31942} FlAsH-EDT2 is commonly used to study protein trafficking, folding, and interactions in living cells or cell lysates.{31942,31940,31941} This green-emitting fluorophore is excited at 508 nm, with emission at 528 nm.{31941}  

     

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    Cayman
    SKU:20704 -

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  • FlAsH-EDT2 is a pro-fluorescent, membrane-permeable biarsenical compound that binds covalently to a tetracysteine sequence (CCPGCC), which is engineered into target proteins.{33065,31942} It binds proteins that have the CCPGCC tag almost immediately after translation.{31942} FlAsH-EDT2 is commonly used to study protein trafficking, folding, and interactions in living cells or cell lysates.{31942,31940,31941} This green-emitting fluorophore is excited at 508 nm, with emission at 528 nm.{31941}  

     

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    Cayman
    SKU:20704 -

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  • FlAsH-EDT2 is a pro-fluorescent, membrane-permeable biarsenical compound that binds covalently to a tetracysteine sequence (CCPGCC), which is engineered into target proteins.{33065,31942} It binds proteins that have the CCPGCC tag almost immediately after translation.{31942} FlAsH-EDT2 is commonly used to study protein trafficking, folding, and interactions in living cells or cell lysates.{31942,31940,31941} This green-emitting fluorophore is excited at 508 nm, with emission at 528 nm.{31941}  

     

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    Cayman
    SKU:20704 -

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  • FlAsH-EDT2 is a pro-fluorescent, membrane-permeable biarsenical compound that binds covalently to a tetracysteine sequence (CCPGCC), which is engineered into target proteins.{33065,31942} It binds proteins that have the CCPGCC tag almost immediately after translation.{31942} FlAsH-EDT2 is commonly used to study protein trafficking, folding, and interactions in living cells or cell lysates.{31942,31940,31941} This green-emitting fluorophore is excited at 508 nm, with emission at 528 nm.{31941}  

     

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    Cayman
    SKU:20704 -

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  • Flavokawain B is a natural chalcone first isolated from extracts of kava roots. It induces apoptosis in androgen receptor-negative, hormone-refractory prostate cancer cell lines (IC50s = 32, 48, 6.2, and 3.9 µM for LAPC4, LNCaP, PC-3, and DU145 cells, respectively, treated for 48 hours), with increased expression of the proapoptotic protein Bim.{31388} Flavokawain B increases Bim expression and inhibits growth of DU145 xenografts in mice.{31388} It also increases Bim expression, promotes apoptosis, and induces cell cycle arrest in uterine leiomyosarcoma cells.{31387} However, flavokawain B is hepatotoxic, triggering oxidative stress, inhibiting NF-κB signaling, and activating MAPK pathways, culminating in HepG2 and L-02 cell death (LD50s = 15 and 32 µM, respectively).{31389}  

     

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    Cayman
    SKU:19652 -

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  • Flavokawain B is a natural chalcone first isolated from extracts of kava roots. It induces apoptosis in androgen receptor-negative, hormone-refractory prostate cancer cell lines (IC50s = 32, 48, 6.2, and 3.9 µM for LAPC4, LNCaP, PC-3, and DU145 cells, respectively, treated for 48 hours), with increased expression of the proapoptotic protein Bim.{31388} Flavokawain B increases Bim expression and inhibits growth of DU145 xenografts in mice.{31388} It also increases Bim expression, promotes apoptosis, and induces cell cycle arrest in uterine leiomyosarcoma cells.{31387} However, flavokawain B is hepatotoxic, triggering oxidative stress, inhibiting NF-κB signaling, and activating MAPK pathways, culminating in HepG2 and L-02 cell death (LD50s = 15 and 32 µM, respectively).{31389}  

     

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    Cayman
    SKU:19652 -

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  • Flavokawain B is a natural chalcone first isolated from extracts of kava roots. It induces apoptosis in androgen receptor-negative, hormone-refractory prostate cancer cell lines (IC50s = 32, 48, 6.2, and 3.9 µM for LAPC4, LNCaP, PC-3, and DU145 cells, respectively, treated for 48 hours), with increased expression of the proapoptotic protein Bim.{31388} Flavokawain B increases Bim expression and inhibits growth of DU145 xenografts in mice.{31388} It also increases Bim expression, promotes apoptosis, and induces cell cycle arrest in uterine leiomyosarcoma cells.{31387} However, flavokawain B is hepatotoxic, triggering oxidative stress, inhibiting NF-κB signaling, and activating MAPK pathways, culminating in HepG2 and L-02 cell death (LD50s = 15 and 32 µM, respectively).{31389}  

     

    Brand:
    Cayman
    SKU:19652 -

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  • Flavokawain B is a natural chalcone first isolated from extracts of kava roots. It induces apoptosis in androgen receptor-negative, hormone-refractory prostate cancer cell lines (IC50s = 32, 48, 6.2, and 3.9 µM for LAPC4, LNCaP, PC-3, and DU145 cells, respectively, treated for 48 hours), with increased expression of the proapoptotic protein Bim.{31388} Flavokawain B increases Bim expression and inhibits growth of DU145 xenografts in mice.{31388} It also increases Bim expression, promotes apoptosis, and induces cell cycle arrest in uterine leiomyosarcoma cells.{31387} However, flavokawain B is hepatotoxic, triggering oxidative stress, inhibiting NF-κB signaling, and activating MAPK pathways, culminating in HepG2 and L-02 cell death (LD50s = 15 and 32 µM, respectively).{31389}  

     

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    Cayman
    SKU:19652 -

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  • Flavopiridol is an orally bioavailable inhibitor of cyclin dependent kinases (IC50s = ~100, ~100, ~100, and 300 nM for Cdk1, Cdk2, Cdk4, and Cdk7, respectively).{23163} It also inhibits TEFb, a complex composed of Cdk9 and cyclin T1, with a Ki value of 3 nM.{23157} Flavopiridol inhibits transcription of a CMV promoter in HeLa nuclear extract (IC50 = 34 nM), Tat-stimulated transcription of an HIV-1 promotor (IC50 = 7 nM), and HIV-1 replication in HEK293T cells (IC50 = In vivo, flavopiridol (5 mg/kg, i.p.) induces apoptosis and cyclin D1 depletion and delays tumor growth in an HN-12 head and neck carcinoma mouse xenograft model.{23163} It also suppresses synovial hyperplasia and joint destruction in a mouse model of collagen-induced arthritis.{23156}  

     

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    Cayman
    SKU:26024 - 100 mg

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  • Flavopiridol is an orally bioavailable inhibitor of cyclin dependent kinases (IC50s = ~100, ~100, ~100, and 300 nM for Cdk1, Cdk2, Cdk4, and Cdk7, respectively).{23163} It also inhibits TEFb, a complex composed of Cdk9 and cyclin T1, with a Ki value of 3 nM.{23157} Flavopiridol inhibits transcription of a CMV promoter in HeLa nuclear extract (IC50 = 34 nM), Tat-stimulated transcription of an HIV-1 promotor (IC50 = 7 nM), and HIV-1 replication in HEK293T cells (IC50 = In vivo, flavopiridol (5 mg/kg, i.p.) induces apoptosis and cyclin D1 depletion and delays tumor growth in an HN-12 head and neck carcinoma mouse xenograft model.{23163} It also suppresses synovial hyperplasia and joint destruction in a mouse model of collagen-induced arthritis.{23156}  

     

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    Cayman
    SKU:26024 - 25 mg

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  • Flavopiridol is an orally bioavailable inhibitor of cyclin dependent kinases (IC50s = ~100, ~100, ~100, and 300 nM for Cdk1, Cdk2, Cdk4, and Cdk7, respectively).{23163} It also inhibits TEFb, a complex composed of Cdk9 and cyclin T1, with a Ki value of 3 nM.{23157} Flavopiridol inhibits transcription of a CMV promoter in HeLa nuclear extract (IC50 = 34 nM), Tat-stimulated transcription of an HIV-1 promotor (IC50 = 7 nM), and HIV-1 replication in HEK293T cells (IC50 = In vivo, flavopiridol (5 mg/kg, i.p.) induces apoptosis and cyclin D1 depletion and delays tumor growth in an HN-12 head and neck carcinoma mouse xenograft model.{23163} It also suppresses synovial hyperplasia and joint destruction in a mouse model of collagen-induced arthritis.{23156}  

     

    Brand:
    Cayman
    SKU:26024 - 5 mg

    Available on backorder

  • Flavopiridol is an orally bioavailable inhibitor of cyclin dependent kinases (IC50s = ~100, ~100, ~100, and 300 nM for Cdk1, Cdk2, Cdk4, and Cdk7, respectively).{23163} It also inhibits TEFb, a complex composed of Cdk9 and cyclin T1, with a Ki value of 3 nM.{23157} Flavopiridol inhibits transcription of a CMV promoter in HeLa nuclear extract (IC50 = 34 nM), Tat-stimulated transcription of an HIV-1 promotor (IC50 = 7 nM), and HIV-1 replication in HEK293T cells (IC50 = In vivo, flavopiridol (5 mg/kg, i.p.) induces apoptosis and cyclin D1 depletion and delays tumor growth in an HN-12 head and neck carcinoma mouse xenograft model.{23163} It also suppresses synovial hyperplasia and joint destruction in a mouse model of collagen-induced arthritis.{23156}  

     

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    Cayman
    SKU:26024 - 50 mg

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  • Flavopiridol is an orally bioavailable inhibitor of cyclin dependent kinases (IC50s = ~100, ~100, ~100, and 300 nM for Cdk1, Cdk2, Cdk4, and Cdk7, respectively).{23163} It also inhibits TEFb, a complex composed of Cdk9 and cyclin T1, with a Ki value of 3 nM.{23157} Flavopiridol inhibits transcription of a CMV promoter in HeLa nuclear extract (IC50 = 34 nM), Tat-stimulated transcription of an HIV-1 promotor (IC50 = 7 nM), and HIV-1 replication in HEK239T cells (IC50 = In vivo, flavopiridol (5 mg/kg, i.p.) induces apoptosis and cyclin D1 depletion and delays tumor growth in an HN-12 head and neck carcinoma mouse xenograft model.{23163} It also suppresses synovial hyperplasia and joint destruction in a mouse model of collagen-induced arthritis.{23156}  

     

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    Cayman
    SKU:10009197 - 10 mg

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  • Flavopiridol is an orally bioavailable inhibitor of cyclin dependent kinases (IC50s = ~100, ~100, ~100, and 300 nM for Cdk1, Cdk2, Cdk4, and Cdk7, respectively).{23163} It also inhibits TEFb, a complex composed of Cdk9 and cyclin T1, with a Ki value of 3 nM.{23157} Flavopiridol inhibits transcription of a CMV promoter in HeLa nuclear extract (IC50 = 34 nM), Tat-stimulated transcription of an HIV-1 promotor (IC50 = 7 nM), and HIV-1 replication in HEK239T cells (IC50 = In vivo, flavopiridol (5 mg/kg, i.p.) induces apoptosis and cyclin D1 depletion and delays tumor growth in an HN-12 head and neck carcinoma mouse xenograft model.{23163} It also suppresses synovial hyperplasia and joint destruction in a mouse model of collagen-induced arthritis.{23156}  

     

    Brand:
    Cayman
    SKU:10009197 - 25 mg

    Available on backorder

  • Flavopiridol is an orally bioavailable inhibitor of cyclin dependent kinases (IC50s = ~100, ~100, ~100, and 300 nM for Cdk1, Cdk2, Cdk4, and Cdk7, respectively).{23163} It also inhibits TEFb, a complex composed of Cdk9 and cyclin T1, with a Ki value of 3 nM.{23157} Flavopiridol inhibits transcription of a CMV promoter in HeLa nuclear extract (IC50 = 34 nM), Tat-stimulated transcription of an HIV-1 promotor (IC50 = 7 nM), and HIV-1 replication in HEK239T cells (IC50 = In vivo, flavopiridol (5 mg/kg, i.p.) induces apoptosis and cyclin D1 depletion and delays tumor growth in an HN-12 head and neck carcinoma mouse xenograft model.{23163} It also suppresses synovial hyperplasia and joint destruction in a mouse model of collagen-induced arthritis.{23156}  

     

    Brand:
    Cayman
    SKU:10009197 - 5 mg

    Available on backorder

  • Flavopiridol is an orally bioavailable inhibitor of cyclin dependent kinases (IC50s = ~100, ~100, ~100, and 300 nM for Cdk1, Cdk2, Cdk4, and Cdk7, respectively).{23163} It also inhibits TEFb, a complex composed of Cdk9 and cyclin T1, with a Ki value of 3 nM.{23157} Flavopiridol inhibits transcription of a CMV promoter in HeLa nuclear extract (IC50 = 34 nM), Tat-stimulated transcription of an HIV-1 promotor (IC50 = 7 nM), and HIV-1 replication in HEK239T cells (IC50 = In vivo, flavopiridol (5 mg/kg, i.p.) induces apoptosis and cyclin D1 depletion and delays tumor growth in an HN-12 head and neck carcinoma mouse xenograft model.{23163} It also suppresses synovial hyperplasia and joint destruction in a mouse model of collagen-induced arthritis.{23156}  

     

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    Cayman
    SKU:10009197 - 50 mg

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  • Flavoxate blocks L-type calcium (Cav1.2) channels and acts an antagonist of muscarinic acetylcholine receptors. Through these actions, flavoxate inhibits contraction of detrusor myocytes and prevents activation of the micturition center in the brain, resulting in muscle relaxation (IC50 = 2 µM for relaxation of human bladder precontracted by K+).{30978} Flavoxate has been studied clinically for the management of overactive bladder, for its potential to relax urinary bladder smooth muscle in order to suppress the micturition reflex.{30978}  

     

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    Cayman
    SKU:-

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  • Flavoxate blocks L-type calcium (Cav1.2) channels and acts an antagonist of muscarinic acetylcholine receptors. Through these actions, flavoxate inhibits contraction of detrusor myocytes and prevents activation of the micturition center in the brain, resulting in muscle relaxation (IC50 = 2 µM for relaxation of human bladder precontracted by K+).{30978} Flavoxate has been studied clinically for the management of overactive bladder, for its potential to relax urinary bladder smooth muscle in order to suppress the micturition reflex.{30978}  

     

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    Cayman
    SKU:-

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  • Flavoxate blocks L-type calcium (Cav1.2) channels and acts an antagonist of muscarinic acetylcholine receptors. Through these actions, flavoxate inhibits contraction of detrusor myocytes and prevents activation of the micturition center in the brain, resulting in muscle relaxation (IC50 = 2 µM for relaxation of human bladder precontracted by K+).{30978} Flavoxate has been studied clinically for the management of overactive bladder, for its potential to relax urinary bladder smooth muscle in order to suppress the micturition reflex.{30978}  

     

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    Cayman
    SKU:-

    Available on backorder