Cayman

Showing 34501–34650 of 45550 results

  • Advanced glycation end products (AGEs) are compounds formed by non-enzymatic chemical reactions following the bonding of sugars to proteins or lipids during diabetes, uremia, aging, rheumatic arthritis, and other conditions. A receptor for the AGEs (RAGE) binds certain members of this class to initiate cell signaling.{17862,17863} Pentosidine is a well-characterized natural AGE that is often used as a biomarker for the production of all AGEs. While pentosidine can be measured in urine, the majority of this AGE is catabolized before excretion.{17864}  

     

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    Cayman
    SKU:10010254 - 5 mg

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  • Because of their antitumor activity via inhibition of DNA synthesis, purine nucleoside derivatives resistant to deamination have been developed for the treatment of various leukemias.{22555,21535} Pentostatin is a purine nucleoside analog that irreversibly inhibits adenosine deaminase (Ki = 0.9 pM) and thus interrupts DNA synthesis in dividing cells.{23726,23725} Pentostatin has been reported to display strong efficacy in the clinical treatment of hairy cell leukemia as well as relapsed chronic lymphocytic leukemia.{23725,21535}  

     

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  • Because of their antitumor activity via inhibition of DNA synthesis, purine nucleoside derivatives resistant to deamination have been developed for the treatment of various leukemias.{22555,21535} Pentostatin is a purine nucleoside analog that irreversibly inhibits adenosine deaminase (Ki = 0.9 pM) and thus interrupts DNA synthesis in dividing cells.{23726,23725} Pentostatin has been reported to display strong efficacy in the clinical treatment of hairy cell leukemia as well as relapsed chronic lymphocytic leukemia.{23725,21535}  

     

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    Cayman
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  • Because of their antitumor activity via inhibition of DNA synthesis, purine nucleoside derivatives resistant to deamination have been developed for the treatment of various leukemias.{22555,21535} Pentostatin is a purine nucleoside analog that irreversibly inhibits adenosine deaminase (Ki = 0.9 pM) and thus interrupts DNA synthesis in dividing cells.{23726,23725} Pentostatin has been reported to display strong efficacy in the clinical treatment of hairy cell leukemia as well as relapsed chronic lymphocytic leukemia.{23725,21535}  

     

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    Cayman
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  • Pentylenetetrazole (PTZ) is a central nervous system modulator that is used to experimentally induce seizures in animals.{30232} Subcutaneous PTZ has been used extensively to screen for compounds that block the production of nonconvulsive (absence or myoclonic) seizures.{17321,23990} PTZ has diverse, site-specific effects in the brain. However, it is an antagonist of GABAA receptors and some drugs that block PTZ-induced seizures, including benzodiazepines, act at the GABAA receptor.{30231,30233}  

     

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  • Peonidin is an O-methylated anthocyanidin that functions as a primary plant pigment, endowing purplish-red hues to flowers such as the peony, from which it takes its name, as well as berries and vegetables. It has been shown to exhibit chemopreventive, as well as anti-inflammatory activities on cancer cells in vitro, blocking COX-2 expression and transformation in JB6 P+ mouse epidermal cells.{31839}  

     

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    Cayman
    SKU:19754 -

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  • Peonidin is an O-methylated anthocyanidin that functions as a primary plant pigment, endowing purplish-red hues to flowers such as the peony, from which it takes its name, as well as berries and vegetables. It has been shown to exhibit chemopreventive, as well as anti-inflammatory activities on cancer cells in vitro, blocking COX-2 expression and transformation in JB6 P+ mouse epidermal cells.{31839}  

     

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    Cayman
    SKU:19754 -

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  • Peonidin is an O-methylated anthocyanidin that functions as a primary plant pigment, endowing purplish-red hues to flowers such as the peony, from which it takes its name, as well as berries and vegetables. It has been shown to exhibit chemopreventive, as well as anti-inflammatory activities on cancer cells in vitro, blocking COX-2 expression and transformation in JB6 P+ mouse epidermal cells.{31839}  

     

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    SKU:19754 -

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  • Peonidin 3-O-glucoside is a metabolite of cyanidin 3-glucoside (Item No. 16406) and an anthocyanin that has been found in red wine extracts and has diverse biological activities, including antioxidant, anti-inflammatory, antiproliferative, and anti-metastatic properties.{42980,42976,42977,42978,42979} Peonidin 3-O-glucoside scavenges 2,2-diphenyl 1-picylhydrazyl (DPPH; Item No. 14805) and ABTS (Item No. 27317) radicals in cell-free assays (EC50s = 757 and 98 μM, respectively).{42976} It inhibits IL-1β-induced phosphorylation of IKKα, IκBα, and ERK in human articular chondrocytes when used at a concentration of 2.5 μM.{42977} Peonidin 3-O-glucoside inhibits the growth of Hs578T human breast cancer cells in vitro in a concentration-dependent manner and decreases pulmonary metastasis in a mouse model of Lewis lung carcinoma when administered at a dose of 20 mg/kg.{42978,42979}  

     

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    SKU:28743 - 1 mg

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  • Peonidin 3-O-glucoside is a metabolite of cyanidin 3-glucoside (Item No. 16406) and an anthocyanin that has been found in red wine extracts and has diverse biological activities, including antioxidant, anti-inflammatory, antiproliferative, and anti-metastatic properties.{42980,42976,42977,42978,42979} Peonidin 3-O-glucoside scavenges 2,2-diphenyl 1-picylhydrazyl (DPPH; Item No. 14805) and ABTS (Item No. 27317) radicals in cell-free assays (EC50s = 757 and 98 μM, respectively).{42976} It inhibits IL-1β-induced phosphorylation of IKKα, IκBα, and ERK in human articular chondrocytes when used at a concentration of 2.5 μM.{42977} Peonidin 3-O-glucoside inhibits the growth of Hs578T human breast cancer cells in vitro in a concentration-dependent manner and decreases pulmonary metastasis in a mouse model of Lewis lung carcinoma when administered at a dose of 20 mg/kg.{42978,42979}  

     

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    SKU:28743 - 5 mg

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  • PEPA is a positive allosteric modulator (PAM) of AMPA receptors.{52115} It selectively increases glutamate-induced currents in X. laevis oocytes expressing the flop isoforms of the AMPA receptor subunits glutamate receptor 3 (GluR3) and GluR4 over the flip isoforms of these subunits at 200 µM. PEPA (10 mg/kg) decreases the latency to find the platform in the Morris water maze, indicating reversal of memory deficits, in a rat model of memory impairment induced by middle cerebral artery occlusion (MCAO).{52116} It decreases freezing time in a contextual fear freezing paradigm in mice when administered at a dose of 30 mg/kg.{52117}  

     

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    Cayman
    SKU:29190 - 10 mg

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  • PEPA is a positive allosteric modulator (PAM) of AMPA receptors.{52115} It selectively increases glutamate-induced currents in X. laevis oocytes expressing the flop isoforms of the AMPA receptor subunits glutamate receptor 3 (GluR3) and GluR4 over the flip isoforms of these subunits at 200 µM. PEPA (10 mg/kg) decreases the latency to find the platform in the Morris water maze, indicating reversal of memory deficits, in a rat model of memory impairment induced by middle cerebral artery occlusion (MCAO).{52116} It decreases freezing time in a contextual fear freezing paradigm in mice when administered at a dose of 30 mg/kg.{52117}  

     

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    SKU:29190 - 5 mg

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  • Immunoge: Peptide from the N-terminal region of mouse PEPCK · Host: Rabbit · Species Reactivity: (+) mouse and rat PEPCK protein · Application(s): WB • PEPCK catalyzes the conversion of oxaloacetate to phosphoenolpyruvate, the first committed step in gluconeogenesis. Both non-insulin-dependent diabetes mellitus and streptozotocin-induced diabetes result in elevated PEPCK activity, protein, and mRNA. This antibody was generated against mouse cytosolic PEPCK.  

     

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    SKU:10004943- 1 ea

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  • Immunoge: Peptide from the N-terminal region of mouse PEPCK · Host: Rabbit · Species Reactivity: (+) mouse and rat PEPCK protein · Application(s): WB • PEPCK catalyzes the conversion of oxaloacetate to phosphoenolpyruvate, the first committed step in gluconeogenesis. Both non-insulin-dependent diabetes mellitus and streptozotocin-induced diabetes result in elevated PEPCK activity, protein, and mRNA. This antibody was generated against mouse cytosolic PEPCK.  

     

    Brand:
    Cayman
    SKU:10004943- 1 ea
  • Phosphoenolpyruvate carboxykinase (PEPCK) is a hormonally regulated enzyme responsible for the first committed step in gluconeogenesis, catalyzing the conversion of oxaloacetate to phosphoenolpyruvate.{13231,13234} PEPCK mRNA is most abundant in the liver, kidney cortex, and white adipose tissue but is also found in brown fat, the mammary gland during lactation, and the small intestine.{13234} Both non-insulin-dependent diabetes mellitus and streptozotocin-induced diabetes result in elevated PEPCK activity, protein, and mRNA.{13231,13237} Two isozymes of PEPCK have been identified, cytosolic and mitochondrial.{13240} Cayman’s PEPCK polyclonal antibody was generated against murine cytosolic PEPCK and detects the protein at 63 kDa by western blotting in rat and murine samples.  

     

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    SKU:10004943 - 1 ea

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  • Pepstatin A is a bacterial-derived chemotactic pentapeptide that irreversibly inhibits aspartic proteases, including pepsin, gastricsin, renin, cathepsin E, and cathepsin D.{23717} Pepstatin A has been reported to stimulate human neutrophil degranulation (EC50 = 0.75 μM) and super oxide production (EC50 = 1.5 μM).{23718} Pepstatin A has been widely used as a research tool in studies of protease mechanisms and biological functions and has been examined as a therapeutic agent for inflammatory conditions including gastric ulcer, edema, and hypertension.{23716}  

     

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    Cayman
    SKU:9000469 - 10 mg

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  • Pepstatin A is a bacterial-derived chemotactic pentapeptide that irreversibly inhibits aspartic proteases, including pepsin, gastricsin, renin, cathepsin E, and cathepsin D.{23717} Pepstatin A has been reported to stimulate human neutrophil degranulation (EC50 = 0.75 μM) and super oxide production (EC50 = 1.5 μM).{23718} Pepstatin A has been widely used as a research tool in studies of protease mechanisms and biological functions and has been examined as a therapeutic agent for inflammatory conditions including gastric ulcer, edema, and hypertension.{23716}  

     

    Brand:
    Cayman
    SKU:9000469 - 25 mg

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  • Pepstatin A is a bacterial-derived chemotactic pentapeptide that irreversibly inhibits aspartic proteases, including pepsin, gastricsin, renin, cathepsin E, and cathepsin D.{23717} Pepstatin A has been reported to stimulate human neutrophil degranulation (EC50 = 0.75 μM) and super oxide production (EC50 = 1.5 μM).{23718} Pepstatin A has been widely used as a research tool in studies of protease mechanisms and biological functions and has been examined as a therapeutic agent for inflammatory conditions including gastric ulcer, edema, and hypertension.{23716}  

     

    Brand:
    Cayman
    SKU:9000469 - 5 mg

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  • Pepstatin A is a bacterial-derived chemotactic pentapeptide that irreversibly inhibits aspartic proteases, including pepsin, gastricsin, renin, cathepsin E, and cathepsin D.{23717} Pepstatin A has been reported to stimulate human neutrophil degranulation (EC50 = 0.75 μM) and super oxide production (EC50 = 1.5 μM).{23718} Pepstatin A has been widely used as a research tool in studies of protease mechanisms and biological functions and has been examined as a therapeutic agent for inflammatory conditions including gastric ulcer, edema, and hypertension.{23716}  

     

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    Cayman
    SKU:9000469 - 50 mg

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  • Peptide YY (PYY) is a polypeptide that is released postprandially in proportion to meal energy content by endocrine L cells in the ileum and colon in order to regulate appetite.{24276} PYY, along with neuropeptide Y (NPY; Item No. 15071), inhibits gastrointestinal motility and electrolyte secretion, which is thought to indicate satiety through a potent feedback signal on hypothalamic circuits.{24276,27059} Upon release, PYY is cleaved to PYY (3-36), which is a preferred agonist at presynaptic inhibitory type 2 NPY autoreceptors (EC50 = 11.4 nM in human colon mucosa).{27058} PYY (3-36) has been associated with dose-dependent weight loss in various obesity models including ob/ob mice, diet-induced obese mice, and non-diabetic fatty Zucker rats.{27059}  

     

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  • Peptide YY (PYY) is a polypeptide that is released postprandially in proportion to meal energy content by endocrine L cells in the ileum and colon in order to regulate appetite.{24276} PYY, along with neuropeptide Y (NPY; Item No. 15071), inhibits gastrointestinal motility and electrolyte secretion, which is thought to indicate satiety through a potent feedback signal on hypothalamic circuits.{24276,27059} Upon release, PYY is cleaved to PYY (3-36), which is a preferred agonist at presynaptic inhibitory type 2 NPY autoreceptors (EC50 = 11.4 nM in human colon mucosa).{27058} PYY (3-36) has been associated with dose-dependent weight loss in various obesity models including ob/ob mice, diet-induced obese mice, and non-diabetic fatty Zucker rats.{27059}  

     

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  • Peramivir is an inhibitor of influenza neuraminidase (IC50s = 0.09 and 11 nM for influenza A and B neuraminidases, respectively).{41314} It is selective for influenza neuraminidase over bacterial, mammalian, and other viral neuraminidases (IC50s = >300 μM). Peramivir inhibits neuraminidase activity in H1N1, H2N2, H3N2, and H6N2 influenza strains (IC50s = 0.09-1.1 nM) and reduces lysis of MDCK cells infected with influenza (EC50s = <0.01-21 nM). Pretreatment with peramivir (10-100 mg/kg) protects mice against lethal influenza infections. It also increases survival in ferrets infected intranasally with avian influenza type A H5N1 when injected intramuscularly after infection.{41315} Formulations containing peramivir have been used to treat influenza.  

     

    Brand:
    Cayman
    SKU:23765 - 1 mg

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  • Peramivir is an inhibitor of influenza neuraminidase (IC50s = 0.09 and 11 nM for influenza A and B neuraminidases, respectively).{41314} It is selective for influenza neuraminidase over bacterial, mammalian, and other viral neuraminidases (IC50s = >300 μM). Peramivir inhibits neuraminidase activity in H1N1, H2N2, H3N2, and H6N2 influenza strains (IC50s = 0.09-1.1 nM) and reduces lysis of MDCK cells infected with influenza (EC50s = <0.01-21 nM). Pretreatment with peramivir (10-100 mg/kg) protects mice against lethal influenza infections. It also increases survival in ferrets infected intranasally with avian influenza type A H5N1 when injected intramuscularly after infection.{41315} Formulations containing peramivir have been used to treat influenza.  

     

    Brand:
    Cayman
    SKU:23765 - 10 mg

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  • Peramivir is an inhibitor of influenza neuraminidase (IC50s = 0.09 and 11 nM for influenza A and B neuraminidases, respectively).{41314} It is selective for influenza neuraminidase over bacterial, mammalian, and other viral neuraminidases (IC50s = >300 μM). Peramivir inhibits neuraminidase activity in H1N1, H2N2, H3N2, and H6N2 influenza strains (IC50s = 0.09-1.1 nM) and reduces lysis of MDCK cells infected with influenza (EC50s = <0.01-21 nM). Pretreatment with peramivir (10-100 mg/kg) protects mice against lethal influenza infections. It also increases survival in ferrets infected intranasally with avian influenza type A H5N1 when injected intramuscularly after infection.{41315} Formulations containing peramivir have been used to treat influenza.  

     

    Brand:
    Cayman
    SKU:23765 - 25 mg

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  • Peramivir is an inhibitor of influenza neuraminidase (IC50s = 0.09 and 11 nM for influenza A and B neuraminidases, respectively).{41314} It is selective for influenza neuraminidase over bacterial, mammalian, and other viral neuraminidases (IC50s = >300 μM). Peramivir inhibits neuraminidase activity in H1N1, H2N2, H3N2, and H6N2 influenza strains (IC50s = 0.09-1.1 nM) and reduces lysis of MDCK cells infected with influenza (EC50s = <0.01-21 nM). Pretreatment with peramivir (10-100 mg/kg) protects mice against lethal influenza infections. It also increases survival in ferrets infected intranasally with avian influenza type A H5N1 when injected intramuscularly after infection.{41315} Formulations containing peramivir have been used to treat influenza.  

     

    Brand:
    Cayman
    SKU:23765 - 5 mg

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  • Pergolide is a potent dopamine D1 and D2 receptor agonist (Kis = 111 and 0.495 nM, respectively, for rat striatal receptors).{41336} It depresses dopaminergic firing in paralyzed rats (ED50 = 2-selective antagonist spiperone or the dopamine D1-selective antagonist SCH 23390 (Item No. 15631).{42504} Pergolide (0.025 and 0.05 mg/kg) increases the volume threshold for inducing bladder contraction in a cynomolgus monkey model of Parkinson’s disease induced by MPTP.{42505} It also reduces carrageenan-induced paw edema in adrenalectomized rats (ED50 = 0.4 mg/kg).{42506}  

     

    Brand:
    Cayman
    SKU:26085 - 100 mg

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  • Pergolide is a potent dopamine D1 and D2 receptor agonist (Kis = 111 and 0.495 nM, respectively, for rat striatal receptors).{41336} It depresses dopaminergic firing in paralyzed rats (ED50 = 2-selective antagonist spiperone or the dopamine D1-selective antagonist SCH 23390 (Item No. 15631).{42504} Pergolide (0.025 and 0.05 mg/kg) increases the volume threshold for inducing bladder contraction in a cynomolgus monkey model of Parkinson’s disease induced by MPTP.{42505} It also reduces carrageenan-induced paw edema in adrenalectomized rats (ED50 = 0.4 mg/kg).{42506}  

     

    Brand:
    Cayman
    SKU:26085 - 25 mg

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  • Pergolide is a potent dopamine D1 and D2 receptor agonist (Kis = 111 and 0.495 nM, respectively, for rat striatal receptors).{41336} It depresses dopaminergic firing in paralyzed rats (ED50 = 2-selective antagonist spiperone or the dopamine D1-selective antagonist SCH 23390 (Item No. 15631).{42504} Pergolide (0.025 and 0.05 mg/kg) increases the volume threshold for inducing bladder contraction in a cynomolgus monkey model of Parkinson’s disease induced by MPTP.{42505} It also reduces carrageenan-induced paw edema in adrenalectomized rats (ED50 = 0.4 mg/kg).{42506}  

     

    Brand:
    Cayman
    SKU:26085 - 250 mg

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  • Pergolide is a potent dopamine D1 and D2 receptor agonist (Kis = 111 and 0.495 nM, respectively, for rat striatal receptors).{41336} It depresses dopaminergic firing in paralyzed rats (ED50 = 2-selective antagonist spiperone or the dopamine D1-selective antagonist SCH 23390 (Item No. 15631).{42504} Pergolide (0.025 and 0.05 mg/kg) increases the volume threshold for inducing bladder contraction in a cynomolgus monkey model of Parkinson’s disease induced by MPTP.{42505} It also reduces carrageenan-induced paw edema in adrenalectomized rats (ED50 = 0.4 mg/kg).{42506}  

     

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    Cayman
    SKU:26085 - 50 mg

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  • Perhexiline is a carnitine palmitoyltransferase 1 (CPT1) and CPT2 inhibitor that was originally developed as an anti-anginal drug in the 1970s.{28039,28040,28041} It inhibits rat heart and liver CPT1 (IC50 = 77 and 148 µM, respectively) and rat heart CPT2 (IC50 = 79 µM).{28039,28040} Inhibition of CPT reduces uptake of long-chain fatty acids into the mitochondria, thereby shifting cellular metabolism from β-oxidation to glycolysis. Perhexilin inhibits mTORC1 signaling at 10 µM and induces autophagy ~7-fold at a concentration of 10 µM in MCF-7 cells.{17472}  

     

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  • Perhexiline is a carnitine palmitoyltransferase 1 (CPT1) and CPT2 inhibitor that was originally developed as an anti-anginal drug in the 1970s.{28039,28040,28041} It inhibits rat heart and liver CPT1 (IC50 = 77 and 148 µM, respectively) and rat heart CPT2 (IC50 = 79 µM).{28039,28040} Inhibition of CPT reduces uptake of long-chain fatty acids into the mitochondria, thereby shifting cellular metabolism from β-oxidation to glycolysis. Perhexilin inhibits mTORC1 signaling at 10 µM and induces autophagy ~7-fold at a concentration of 10 µM in MCF-7 cells.{17472}  

     

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  • Perhexiline is a carnitine palmitoyltransferase 1 (CPT1) and CPT2 inhibitor that was originally developed as an anti-anginal drug in the 1970s.{28039,28040,28041} It inhibits rat heart and liver CPT1 (IC50 = 77 and 148 µM, respectively) and rat heart CPT2 (IC50 = 79 µM).{28039,28040} Inhibition of CPT reduces uptake of long-chain fatty acids into the mitochondria, thereby shifting cellular metabolism from β-oxidation to glycolysis. Perhexilin inhibits mTORC1 signaling at 10 µM and induces autophagy ~7-fold at a concentration of 10 µM in MCF-7 cells.{17472}  

     

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  • Pericosine A is a fungal metabolite that has been found in P. byssoides and has anticancer activity.{49631} It inhibits the growth of a variety of cancer cells, including breast, colon, lung, ovary, stomach, and prostate cell lines (GI50s = 0.05-24.55 µM) and increases survival in a P388 mouse xenograft model when administered at a dose of 25 mg/kg. Pericosine A inhibits EGFR by 40 to 70% when used at a concentration of 100 µg/ml. It also reacts with organosulfur compounds in skunk spray to form stable thioethers as odorless products.{49632}  

     

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    Cayman
    SKU:29633 - 1 mg

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  • Alkylphospholipids are a class of antineoplastic compounds that display potent antiproliferative activity in several in vitro and in vivo human tumor models. Perifosine is an alkylphospholipid that induces apoptotic cell death in a variety of tumor cell lines.{14118} Apoptosis is induced in a time- and dose-dependent manner in U937 and Jurkat T human leukemia cell lines but not in normal vascular endothelial cells. Perifosine causes inhibition of PC-3 prostate carcinoma cell growth (growth inhibition (GI50) = 5 µM at 24 h) and is associated with rapidly decreased Akt activation.{13739} In addition, perifosine induces p21WAF1 expression in squamous carcinoma cells through a p53-independent pathway, leading to loss in cyclin-dependent kinase activity and cell cycle arrest.{14119}  

     

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    Cayman
    SKU:10008112 - 1 mg

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  • Alkylphospholipids are a class of antineoplastic compounds that display potent antiproliferative activity in several in vitro and in vivo human tumor models. Perifosine is an alkylphospholipid that induces apoptotic cell death in a variety of tumor cell lines.{14118} Apoptosis is induced in a time- and dose-dependent manner in U937 and Jurkat T human leukemia cell lines but not in normal vascular endothelial cells. Perifosine causes inhibition of PC-3 prostate carcinoma cell growth (growth inhibition (GI50) = 5 µM at 24 h) and is associated with rapidly decreased Akt activation.{13739} In addition, perifosine induces p21WAF1 expression in squamous carcinoma cells through a p53-independent pathway, leading to loss in cyclin-dependent kinase activity and cell cycle arrest.{14119}  

     

    Brand:
    Cayman
    SKU:10008112 - 10 mg

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  • Alkylphospholipids are a class of antineoplastic compounds that display potent antiproliferative activity in several in vitro and in vivo human tumor models. Perifosine is an alkylphospholipid that induces apoptotic cell death in a variety of tumor cell lines.{14118} Apoptosis is induced in a time- and dose-dependent manner in U937 and Jurkat T human leukemia cell lines but not in normal vascular endothelial cells. Perifosine causes inhibition of PC-3 prostate carcinoma cell growth (growth inhibition (GI50) = 5 µM at 24 h) and is associated with rapidly decreased Akt activation.{13739} In addition, perifosine induces p21WAF1 expression in squamous carcinoma cells through a p53-independent pathway, leading to loss in cyclin-dependent kinase activity and cell cycle arrest.{14119}  

     

    Brand:
    Cayman
    SKU:10008112 - 25 mg

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  • Alkylphospholipids are a class of antineoplastic compounds that display potent antiproliferative activity in several in vitro and in vivo human tumor models. Perifosine is an alkylphospholipid that induces apoptotic cell death in a variety of tumor cell lines.{14118} Apoptosis is induced in a time- and dose-dependent manner in U937 and Jurkat T human leukemia cell lines but not in normal vascular endothelial cells. Perifosine causes inhibition of PC-3 prostate carcinoma cell growth (growth inhibition (GI50) = 5 µM at 24 h) and is associated with rapidly decreased Akt activation.{13739} In addition, perifosine induces p21WAF1 expression in squamous carcinoma cells through a p53-independent pathway, leading to loss in cyclin-dependent kinase activity and cell cycle arrest.{14119}  

     

    Brand:
    Cayman
    SKU:10008112 - 5 mg

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  • Perindopril is an orally active angiotensin converting enzyme (ACE) inhibitor that effectively lowers blood pressure.{29639,29640} It is a prodrug that is metabolized to perindoprilat (Item No. 17574), a specific, competitive inhibitor of ACE (IC50 = 1.5-3.2 nM in vitro).{30687}  

     

    Brand:
    Cayman
    SKU:20796 -

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  • Perindopril is an orally active angiotensin converting enzyme (ACE) inhibitor that effectively lowers blood pressure.{29639,29640} It is a prodrug that is metabolized to perindoprilat (Item No. 17574), a specific, competitive inhibitor of ACE (IC50 = 1.5-3.2 nM in vitro).{30687}  

     

    Brand:
    Cayman
    SKU:20796 -

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  • Perindopril is an orally active angiotensin converting enzyme (ACE) inhibitor that effectively lowers blood pressure.{29639,29640} It is a prodrug that is metabolized to perindoprilat (Item No. 17574), a specific, competitive inhibitor of ACE (IC50 = 1.5-3.2 nM in vitro).{30687}  

     

    Brand:
    Cayman
    SKU:20796 -

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  • Perindopril is an orally active angiotensin converting enzyme (ACE) inhibitor that effectively lowers blood pressure.{29639,29640} It is a prodrug that is metabolized to perindoprilat (Item No. 17574), a specific, competitive inhibitor of ACE (IC50 = 1.5-3.2 nM in vitro).{30687}  

     

    Brand:
    Cayman
    SKU:20796 -

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  • Perindoprilat is the active metabolite of perindopril, an inhibitor of angiotensin converting enzyme (ACE) that has efficacy against hypertension.{29640} Perindoprilat specifically and competitively inhibits ACE in vitro with IC50 values ranging between 1.5 and 3.2 nM. Elimination of perindoprilat is decreased in the elderly and in patients with heart or renal failure.{29640,29639,29638}  

     

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  • Perindoprilat is the active metabolite of perindopril, an inhibitor of angiotensin converting enzyme (ACE) that has efficacy against hypertension.{29640} Perindoprilat specifically and competitively inhibits ACE in vitro with IC50 values ranging between 1.5 and 3.2 nM. Elimination of perindoprilat is decreased in the elderly and in patients with heart or renal failure.{29640,29639,29638}  

     

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    Cayman
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  • Perindoprilat is the active metabolite of perindopril, an inhibitor of angiotensin converting enzyme (ACE) that has efficacy against hypertension.{29640} Perindoprilat specifically and competitively inhibits ACE in vitro with IC50 values ranging between 1.5 and 3.2 nM. Elimination of perindoprilat is decreased in the elderly and in patients with heart or renal failure.{29640,29639,29638}  

     

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  • Periplocin is a cardiac glycoside that has been isolated from P. sepium and has cardiac and anticancer activity.{37618} It increases viability and proliferation of mouse cardiac microvascular endothelial cells (CMECs) when used at concentrations ranging from 2 to 50 µM and improves left ventricular structure and function in a rat model of chronic heart failure.{37621,37622} Periplocin inhibits cell proliferation in nine lung cancer cell lines in a time- and dose-dependent manner with IC50 values ranging from 0.12 to 53 µM.{37619} It induces apoptosis in SGC-7901 and MGC-803 gastric cancer cells and activates the ERK1/2-EGR1 pathway.{37620} Periplocin (5 and 20 mg/kg) reduces tumor growth in a hepatocellular carcinoma (HCC) mouse xenograft model.{37618} It also inhibits AKT and ERK autophosphorylation and tumor growth in an A549 lung cancer mouse xenograft model when administered at doses of 50 and 100 µg.{37619}  

     

    Brand:
    Cayman
    SKU:25216 - 1 mg

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  • Periplocin is a cardiac glycoside that has been isolated from P. sepium and has cardiac and anticancer activity.{37618} It increases viability and proliferation of mouse cardiac microvascular endothelial cells (CMECs) when used at concentrations ranging from 2 to 50 µM and improves left ventricular structure and function in a rat model of chronic heart failure.{37621,37622} Periplocin inhibits cell proliferation in nine lung cancer cell lines in a time- and dose-dependent manner with IC50 values ranging from 0.12 to 53 µM.{37619} It induces apoptosis in SGC-7901 and MGC-803 gastric cancer cells and activates the ERK1/2-EGR1 pathway.{37620} Periplocin (5 and 20 mg/kg) reduces tumor growth in a hepatocellular carcinoma (HCC) mouse xenograft model.{37618} It also inhibits AKT and ERK autophosphorylation and tumor growth in an A549 lung cancer mouse xenograft model when administered at doses of 50 and 100 µg.{37619}  

     

    Brand:
    Cayman
    SKU:25216 - 10 mg

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  • Periplocin is a cardiac glycoside that has been isolated from P. sepium and has cardiac and anticancer activity.{37618} It increases viability and proliferation of mouse cardiac microvascular endothelial cells (CMECs) when used at concentrations ranging from 2 to 50 µM and improves left ventricular structure and function in a rat model of chronic heart failure.{37621,37622} Periplocin inhibits cell proliferation in nine lung cancer cell lines in a time- and dose-dependent manner with IC50 values ranging from 0.12 to 53 µM.{37619} It induces apoptosis in SGC-7901 and MGC-803 gastric cancer cells and activates the ERK1/2-EGR1 pathway.{37620} Periplocin (5 and 20 mg/kg) reduces tumor growth in a hepatocellular carcinoma (HCC) mouse xenograft model.{37618} It also inhibits AKT and ERK autophosphorylation and tumor growth in an A549 lung cancer mouse xenograft model when administered at doses of 50 and 100 µg.{37619}  

     

    Brand:
    Cayman
    SKU:25216 - 5 mg

    Available on backorder

  • Periplocin is a cardiac glycoside that has been isolated from P. sepium and has cardiac and anticancer activity.{37618} It increases viability and proliferation of mouse cardiac microvascular endothelial cells (CMECs) when used at concentrations ranging from 2 to 50 µM and improves left ventricular structure and function in a rat model of chronic heart failure.{37621,37622} Periplocin inhibits cell proliferation in nine lung cancer cell lines in a time- and dose-dependent manner with IC50 values ranging from 0.12 to 53 µM.{37619} It induces apoptosis in SGC-7901 and MGC-803 gastric cancer cells and activates the ERK1/2-EGR1 pathway.{37620} Periplocin (5 and 20 mg/kg) reduces tumor growth in a hepatocellular carcinoma (HCC) mouse xenograft model.{37618} It also inhibits AKT and ERK autophosphorylation and tumor growth in an A549 lung cancer mouse xenograft model when administered at doses of 50 and 100 µg.{37619}  

     

    Brand:
    Cayman
    SKU:25216 - 50 mg

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  • Permethrin is a modulator of voltage-gated sodium channels (NaV) that is used as an insecticide.{36375} It delays channel deactivation of the NaV1.8 channel expressed in X. laevis oocytes. It is at least 100-fold more potent at insect than mammalian sodium channels, leading to slow deactivation of D. para/TipE, but not rat brain IIA or β1, sodium channels expressed in X. laevis oocytes when used at a concentration of 500 nM.{36376} Permethrin (5 µM) increases sodium influx in BV-2 and primary microglial cells by approximately 28 and 29%, respectively, and activates microglia.{36377} Long-term application of permethrin leads to dose- and time-dependent intracellular sodium accumulation and TNF-α release in microglia in vitro. Formulations containing permethrin have been used for the treatment of head lice and scabies infestations.  

     

    Brand:
    Cayman
    SKU:23821 - 100 mg

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  • Peroxynitrite is formed in vivo by the reaction of NO with superoxide.{2738,5439,1678} It is a powerful oxidizing agent that can initiate lipid peroxidation, oxidize sulfhydryls, and nitrate the aromatic residues of proteins.  

     

    Brand:
    Cayman
    SKU:81565 - 1 ml

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  • Peroxynitrite is formed in vivo by the reaction of NO with superoxide.{2738,5439,1678} It is a powerful oxidizing agent that can initiate lipid peroxidation, oxidize sulfhydryls, and nitrate the aromatic residues of proteins.  

     

    Brand:
    Cayman
    SKU:81565 - 5 ml

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  • Perphenazine is a phenothiazine that binds with high affinity to a wide variety of receptors, including dopamine, serotonin (5-HT), histamine, and α-adrenergic receptors (Kis = 1.4, 5.6, 8, 10, and 17 nM for D2, 5-HT2A, H1, α1A, and 5-HT6, respectively).{24253} It is described as a typical antipsychotic and has been used extensively for schizophrenia and schizophrenia-like psychoses.{32677}  

     

    Brand:
    Cayman
    SKU:20735 -

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  • Perphenazine is a phenothiazine that binds with high affinity to a wide variety of receptors, including dopamine, serotonin (5-HT), histamine, and α-adrenergic receptors (Kis = 1.4, 5.6, 8, 10, and 17 nM for D2, 5-HT2A, H1, α1A, and 5-HT6, respectively).{24253} It is described as a typical antipsychotic and has been used extensively for schizophrenia and schizophrenia-like psychoses.{32677}  

     

    Brand:
    Cayman
    SKU:20735 -

    Available on backorder

  • Perphenazine is a phenothiazine that binds with high affinity to a wide variety of receptors, including dopamine, serotonin (5-HT), histamine, and α-adrenergic receptors (Kis = 1.4, 5.6, 8, 10, and 17 nM for D2, 5-HT2A, H1, α1A, and 5-HT6, respectively).{24253} It is described as a typical antipsychotic and has been used extensively for schizophrenia and schizophrenia-like psychoses.{32677}  

     

    Brand:
    Cayman
    SKU:20735 -

    Available on backorder

  • Perphenazine is a phenothiazine that binds with high affinity to a wide variety of receptors, including dopamine, serotonin (5-HT), histamine, and α-adrenergic receptors (Kis = 1.4, 5.6, 8, 10, and 17 nM for D2, 5-HT2A, H1, α1A, and 5-HT6, respectively).{24253} It is described as a typical antipsychotic and has been used extensively for schizophrenia and schizophrenia-like psychoses.{32677}  

     

    Brand:
    Cayman
    SKU:20735 -

    Available on backorder

  • Pertussis toxin (islet-activating protein) is a toxin, first isolated from B. pertussis, that is used to study G protein-coupled receptor signaling in cells and experimental autoimmune encephalomyelitis (EAE) in animals. Pertussis toxin catalyzes the transfer of the ADP-ribose moiety of NAD to the α subunits of heterotrimeric Gi/o proteins, resulting in the receptors being uncoupled from Gi/o proteins.{31502,31505} Pertussis toxin is also used as an adjuvant, given with specific antigens, to immunize animals and induce EAE, an animal model of multiple sclerosis.{31501,31504} Pertussis toxin was first described as an islet-activating protein because it caused a sustained potentiation of the secretory response of pancreatic islet cells to various stimuli that stimulate Gi-linked α-adrenergic receptors.{31500,31503}  

     

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    Cayman
    SKU:-

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  • Pestalotin is a fungal metabolite originally isolated from P. cryptomeriaecola with diverse biological activities.{37633} It induces reducing sugar release in embryoless rice endosperms when used at concentrations ranging from 3 to 100 mg/L and enhances growth of rice seedlings (O. sativa) when used in combination with gibberellin A3 at concentrations ranging from 30 to 500 mg/L. Pestalotin has antifungal activity, reducing the growth of C. albicans, C. neoformans, T. rubrum, and A. fumigatus (MICs = 12.5, 50, 50, and 50 μg/ml, respectively).{37634} It is cytotoxic to HL-60, MKN45, LoVo, and A549 cells (IC50s = 64.87-182.92 μM). Pestalotin has been used as a standard for dereplication of natural products.{41781}  

     

    Brand:
    Cayman
    SKU:25516 - 2.5 mg

    Available on backorder

  • Pestalotin is a fungal metabolite originally isolated from P. cryptomeriaecola with diverse biological activities.{37633} It induces reducing sugar release in embryoless rice endosperms when used at concentrations ranging from 3 to 100 mg/L and enhances growth of rice seedlings (O. sativa) when used in combination with gibberellin A3 at concentrations ranging from 30 to 500 mg/L. Pestalotin has antifungal activity, reducing the growth of C. albicans, C. neoformans, T. rubrum, and A. fumigatus (MICs = 12.5, 50, 50, and 50 μg/ml, respectively).{37634} It is cytotoxic to HL-60, MKN45, LoVo, and A549 cells (IC50s = 64.87-182.92 μM). Pestalotin has been used as a standard for dereplication of natural products.{41781}  

     

    Brand:
    Cayman
    SKU:25516 - 500 µg

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  • Petromurin C is a bis-indolyl benzenoid fungal metabolite originally isolated from the ascostromata of P. muricatus.{36676} It is cytotoxic to NS-1 mouse myeloma cells (IC50 = 33 μg/ml) and has activity against T. foetus in vitro (IC50 = 100 μg/ml).{39715}  

     

    Brand:
    Cayman
    SKU:25089 - 2.5 mg

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  • Petromurin C is a bis-indolyl benzenoid fungal metabolite originally isolated from the ascostromata of P. muricatus.{36676} It is cytotoxic to NS-1 mouse myeloma cells (IC50 = 33 μg/ml) and has activity against T. foetus in vitro (IC50 = 100 μg/ml).{39715}  

     

    Brand:
    Cayman
    SKU:25089 - 500 µg

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  • Petromyzonol is a tetrahydroxy stearol which serves as the primary spawning pheromone in adult sea lamprey. It is produced in the bile of sea lamprey larvae from the bile acid precursor allocholic acid. While the adult sea lamprey is relatively insensitive to petromyzonol itself, the C-24 sulfate ester (petromyzonol sulfate) is a pheromone and a spawning chemoattractant which can be detected at very low concentrations by lamprey olfactory chemoreceptors. Petromyzonol, petromyzonol sulfate, and allocholic acid are all found in water samples from fresh water streams bearing larval lamprey populations.{7478}  

     

    Brand:
    Cayman
    SKU:98250 - 1 mg

    Available on backorder

  • Petromyzonol is a tetrahydroxy stearol which serves as the primary spawning pheromone in adult sea lamprey. It is produced in the bile of sea lamprey larvae from the bile acid precursor allocholic acid. While the adult sea lamprey is relatively insensitive to petromyzonol itself, the C-24 sulfate ester (petromyzonol sulfate) is a pheromone and a spawning chemoattractant which can be detected at very low concentrations by lamprey olfactory chemoreceptors. Petromyzonol, petromyzonol sulfate, and allocholic acid are all found in water samples from fresh water streams bearing larval lamprey populations.{7478}  

     

    Brand:
    Cayman
    SKU:98250 - 10 mg

    Available on backorder

  • Petromyzonol is a tetrahydroxy stearol which serves as the primary spawning pheromone in adult sea lamprey. It is produced in the bile of sea lamprey larvae from the bile acid precursor allocholic acid. While the adult sea lamprey is relatively insensitive to petromyzonol itself, the C-24 sulfate ester (petromyzonol sulfate) is a pheromone and a spawning chemoattractant which can be detected at very low concentrations by lamprey olfactory chemoreceptors. Petromyzonol, petromyzonol sulfate, and allocholic acid are all found in water samples from fresh water streams bearing larval lamprey populations.{7478}  

     

    Brand:
    Cayman
    SKU:98250 - 5 mg

    Available on backorder

  • Petunidin is an O-methylated anthocyanidin derived from delphinidin (Item No. 11012) that imparts blue-red pigments to flowers, fruits, and red wine. It has been shown to bind with and suppress the activity of focal adhesion kinase and to inhibit platelet-derived growth factor-induced aortic smooth muscle cell migration, which may confer a protective effect against atherosclerosis.{31754} Extracts from E. jambolana fruit, which is rich in anthocyanins including petunidin, have been used to suppress the proliferation of an HCT116 colon cancer cell line, as well as colon cancer stem cells.{31753}  

     

    Brand:
    Cayman
    SKU:19755 -

    Available on backorder

  • Petunidin is an O-methylated anthocyanidin derived from delphinidin (Item No. 11012) that imparts blue-red pigments to flowers, fruits, and red wine. It has been shown to bind with and suppress the activity of focal adhesion kinase and to inhibit platelet-derived growth factor-induced aortic smooth muscle cell migration, which may confer a protective effect against atherosclerosis.{31754} Extracts from E. jambolana fruit, which is rich in anthocyanins including petunidin, have been used to suppress the proliferation of an HCT116 colon cancer cell line, as well as colon cancer stem cells.{31753}  

     

    Brand:
    Cayman
    SKU:19755 -

    Available on backorder

  • Petunidin is an O-methylated anthocyanidin derived from delphinidin (Item No. 11012) that imparts blue-red pigments to flowers, fruits, and red wine. It has been shown to bind with and suppress the activity of focal adhesion kinase and to inhibit platelet-derived growth factor-induced aortic smooth muscle cell migration, which may confer a protective effect against atherosclerosis.{31754} Extracts from E. jambolana fruit, which is rich in anthocyanins including petunidin, have been used to suppress the proliferation of an HCT116 colon cancer cell line, as well as colon cancer stem cells.{31753}  

     

    Brand:
    Cayman
    SKU:19755 -

    Available on backorder

  • Petunidin is an O-methylated anthocyanidin derived from delphinidin (Item No. 11012) that imparts blue-red pigments to flowers, fruits, and red wine. It has been shown to bind with and suppress the activity of focal adhesion kinase and to inhibit platelet-derived growth factor-induced aortic smooth muscle cell migration, which may confer a protective effect against atherosclerosis.{31754} Extracts from E. jambolana fruit, which is rich in anthocyanins including petunidin, have been used to suppress the proliferation of an HCT116 colon cancer cell line, as well as colon cancer stem cells.{31753}  

     

    Brand:
    Cayman
    SKU:19755 -

    Available on backorder

  • Petunidin 3-O-glucoside is an anthocyanin that has been found in red grapes and red wines with antiproliferative properties.{43543} It reduces DBTRG-05MG glioblastoma cell growth in a time- and concentration-dependent manner by increasing production of reactive oxygen species (ROS) and Bax protein levels and reducing Bcl-2 and caspase-3 activities. Petunidin 3-O-glucoside also reduces glucose uptake, lactic acid production, and NAD levels in DBTRG-05MG cells.  

     

    Brand:
    Cayman
    SKU:25686 - 1 mg

    Available on backorder

  • Petunidin 3-O-glucoside is an anthocyanin that has been found in red grapes and red wines with antiproliferative properties.{43543} It reduces DBTRG-05MG glioblastoma cell growth in a time- and concentration-dependent manner by increasing production of reactive oxygen species (ROS) and Bax protein levels and reducing Bcl-2 and caspase-3 activities. Petunidin 3-O-glucoside also reduces glucose uptake, lactic acid production, and NAD levels in DBTRG-05MG cells.  

     

    Brand:
    Cayman
    SKU:25686 - 5 mg

    Available on backorder

  • Colony stimulating factor 1 (CSF1) is a cytokine that is involved in the recruitment and activation of tissue macrophages. It exerts these effects by binding to its corresponding receptor tyrosine kinase, the cFMS/CSF1 receptor (CSF1R). Pexidartinib is a brain-penetrant inhibitor of CSF1R, as well as c-Kit and FLT3 (IC50s = 20, 10, and 160 nM in vitro, respectively).{30529} It has been used in combination with paclitaxel (Item No. 10461) to block macrophage recruitment in mammary tumor-bearing mice, thus slowing primary tumor development and metastasis.{30529} Pexidartinib has also been used to block microglial stimulation of glioblastoma invasion in both cell culture and a mouse model of glioblastoma multiforme.{30528}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Colony stimulating factor 1 (CSF1) is a cytokine that is involved in the recruitment and activation of tissue macrophages. It exerts these effects by binding to its corresponding receptor tyrosine kinase, the cFMS/CSF1 receptor (CSF1R). Pexidartinib is a brain-penetrant inhibitor of CSF1R, as well as c-Kit and FLT3 (IC50s = 20, 10, and 160 nM in vitro, respectively).{30529} It has been used in combination with paclitaxel (Item No. 10461) to block macrophage recruitment in mammary tumor-bearing mice, thus slowing primary tumor development and metastasis.{30529} Pexidartinib has also been used to block microglial stimulation of glioblastoma invasion in both cell culture and a mouse model of glioblastoma multiforme.{30528}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Colony stimulating factor 1 (CSF1) is a cytokine that is involved in the recruitment and activation of tissue macrophages. It exerts these effects by binding to its corresponding receptor tyrosine kinase, the cFMS/CSF1 receptor (CSF1R). Pexidartinib is a brain-penetrant inhibitor of CSF1R, as well as c-Kit and FLT3 (IC50s = 20, 10, and 160 nM in vitro, respectively).{30529} It has been used in combination with paclitaxel (Item No. 10461) to block macrophage recruitment in mammary tumor-bearing mice, thus slowing primary tumor development and metastasis.{30529} Pexidartinib has also been used to block microglial stimulation of glioblastoma invasion in both cell culture and a mouse model of glioblastoma multiforme.{30528}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Colony stimulating factor 1 (CSF1) is a cytokine that is involved in the recruitment and activation of tissue macrophages. It exerts these effects by binding to its corresponding receptor tyrosine kinase, the cFMS/CSF1 receptor (CSF1R). Pexidartinib is a brain-penetrant inhibitor of CSF1R, as well as c-Kit and FLT3 (IC50s = 20, 10, and 160 nM in vitro, respectively).{30529} It has been used in combination with paclitaxel (Item No. 10461) to block macrophage recruitment in mammary tumor-bearing mice, thus slowing primary tumor development and metastasis.{30529} Pexidartinib has also been used to block microglial stimulation of glioblastoma invasion in both cell culture and a mouse model of glioblastoma multiforme.{30528}  

     

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    Cayman
    SKU:-

    Available on backorder

  • Pexmetinib is a dual inhibitor of Tie2 and p38 MAPK (IC50s = 1, 26, and 35 nM for Tie2, p38α, and p38β, respectively).{43849} It also inhibits Abl, ARG, FGFR, FLT1, FLT4, Fyn, HCK, LYN, and MINK (IC50s = 4, 10, 28, 47, 42, 41, 26, 25, and 26 nM, respectively). Pexmetinib (0.5 and 1 µM) reduces proliferation of KG-1 and KT-1 leukemic cells in vitro.  

     

    Brand:
    Cayman
    SKU:26187 - 1 mg

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  • Pexmetinib is a dual inhibitor of Tie2 and p38 MAPK (IC50s = 1, 26, and 35 nM for Tie2, p38α, and p38β, respectively).{43849} It also inhibits Abl, ARG, FGFR, FLT1, FLT4, Fyn, HCK, LYN, and MINK (IC50s = 4, 10, 28, 47, 42, 41, 26, 25, and 26 nM, respectively). Pexmetinib (0.5 and 1 µM) reduces proliferation of KG-1 and KT-1 leukemic cells in vitro.  

     

    Brand:
    Cayman
    SKU:26187 - 10 mg

    Available on backorder

  • Pexmetinib is a dual inhibitor of Tie2 and p38 MAPK (IC50s = 1, 26, and 35 nM for Tie2, p38α, and p38β, respectively).{43849} It also inhibits Abl, ARG, FGFR, FLT1, FLT4, Fyn, HCK, LYN, and MINK (IC50s = 4, 10, 28, 47, 42, 41, 26, 25, and 26 nM, respectively). Pexmetinib (0.5 and 1 µM) reduces proliferation of KG-1 and KT-1 leukemic cells in vitro.  

     

    Brand:
    Cayman
    SKU:26187 - 5 mg

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  • PF-01247324 is a blocker of the tetrodotoxin-resistant (TTX-R) sodium channel Nav1.8 (IC50 = 0.19 μM for human Nav1.8).{36846} It is selective for Nav1.8 over Nav1.1, Nav1.2, Nav1.5, and Nav1.7 channels (IC50s = 13, 12.8, 9, and 19 μM, respectively) as well as ether-a-go-go (ERG) potassium channels (IC50 = 30 μM). PF-01247324 blocks Nav1.8 channels in a VSP-FRET assay using HEK293 cells (IC50 = 2.6 μM). In vivo, PF-01247324 (100 mg/kg) reduces phase 2 flinching in a rat model of formalin-induced persistent pain.{36847} It increases latency to lift the inflamed paw and latency to paw withdrawal in rat models of carrageenan-induced thermal hyperalgesia and mechanical hyperalgesia induced by complete Freund’s adjuvant (CFA), respectively.  

     

    Brand:
    Cayman
    SKU:22111 -

    Out of stock

  • PF-01247324 is a blocker of the tetrodotoxin-resistant (TTX-R) sodium channel Nav1.8 (IC50 = 0.19 μM for human Nav1.8).{36846} It is selective for Nav1.8 over Nav1.1, Nav1.2, Nav1.5, and Nav1.7 channels (IC50s = 13, 12.8, 9, and 19 μM, respectively) as well as ether-a-go-go (ERG) potassium channels (IC50 = 30 μM). PF-01247324 blocks Nav1.8 channels in a VSP-FRET assay using HEK293 cells (IC50 = 2.6 μM). In vivo, PF-01247324 (100 mg/kg) reduces phase 2 flinching in a rat model of formalin-induced persistent pain.{36847} It increases latency to lift the inflamed paw and latency to paw withdrawal in rat models of carrageenan-induced thermal hyperalgesia and mechanical hyperalgesia induced by complete Freund’s adjuvant (CFA), respectively.  

     

    Brand:
    Cayman
    SKU:22111 -

    Out of stock

  • PF-01247324 is a blocker of the tetrodotoxin-resistant (TTX-R) sodium channel Nav1.8 (IC50 = 0.19 μM for human Nav1.8).{36846} It is selective for Nav1.8 over Nav1.1, Nav1.2, Nav1.5, and Nav1.7 channels (IC50s = 13, 12.8, 9, and 19 μM, respectively) as well as ether-a-go-go (ERG) potassium channels (IC50 = 30 μM). PF-01247324 blocks Nav1.8 channels in a VSP-FRET assay using HEK293 cells (IC50 = 2.6 μM). In vivo, PF-01247324 (100 mg/kg) reduces phase 2 flinching in a rat model of formalin-induced persistent pain.{36847} It increases latency to lift the inflamed paw and latency to paw withdrawal in rat models of carrageenan-induced thermal hyperalgesia and mechanical hyperalgesia induced by complete Freund’s adjuvant (CFA), respectively.  

     

    Brand:
    Cayman
    SKU:22111 -

    Out of stock

  • PF-01247324 is a blocker of the tetrodotoxin-resistant (TTX-R) sodium channel Nav1.8 (IC50 = 0.19 μM for human Nav1.8).{36846} It is selective for Nav1.8 over Nav1.1, Nav1.2, Nav1.5, and Nav1.7 channels (IC50s = 13, 12.8, 9, and 19 μM, respectively) as well as ether-a-go-go (ERG) potassium channels (IC50 = 30 μM). PF-01247324 blocks Nav1.8 channels in a VSP-FRET assay using HEK293 cells (IC50 = 2.6 μM). In vivo, PF-01247324 (100 mg/kg) reduces phase 2 flinching in a rat model of formalin-induced persistent pain.{36847} It increases latency to lift the inflamed paw and latency to paw withdrawal in rat models of carrageenan-induced thermal hyperalgesia and mechanical hyperalgesia induced by complete Freund’s adjuvant (CFA), respectively.  

     

    Brand:
    Cayman
    SKU:22111 -

    Out of stock

  • PF-03550096 is a synthetic cannabinoid (CB) that selectively targets the peripheral CB2 receptor over the central CB1 receptor (Kis = 7.9 and 1,500 nM for human isoforms, respectively).{28936,28937} It shows similar selectivity for inhibiting forskolin-stimulated cAMP production in CHO cells expressing human CB1 and CB2 receptors (EC50s = 450 and 2.1 nM, respectively).{28937} PF-03550096 is orally bioavailable and significantly reduces colonic pain induced by 2,4,6-trinitrobenzene sulfonic acid in rats.{28937} This product is intended for forensic and research applications.  

     

    Brand:
    Cayman
    SKU:-
  • PF-03550096 is a synthetic cannabinoid (CB) that selectively targets the peripheral CB2 receptor over the central CB1 receptor (Kis = 7.9 and 1,500 nM for human isoforms, respectively).{28936,28937} It shows similar selectivity for inhibiting forskolin-stimulated cAMP production in CHO cells expressing human CB1 and CB2 receptors (EC50s = 450 and 2.1 nM, respectively).{28937} PF-03550096 is orally bioavailable and significantly reduces colonic pain induced by 2,4,6-trinitrobenzene sulfonic acid in rats.{28937} This product is intended for forensic and research applications.  

     

    Brand:
    Cayman
    SKU:-
  • PF-03550096 is a synthetic cannabinoid (CB) that selectively targets the peripheral CB2 receptor over the central CB1 receptor (Kis = 7.9 and 1,500 nM for human isoforms, respectively).{28936,28937} It shows similar selectivity for inhibiting forskolin-stimulated cAMP production in CHO cells expressing human CB1 and CB2 receptors (EC50s = 450 and 2.1 nM, respectively).{28937} PF-03550096 is orally bioavailable and significantly reduces colonic pain induced by 2,4,6-trinitrobenzene sulfonic acid in rats.{28937} This product is intended for forensic and research applications.  

     

    Brand:
    Cayman
    SKU:-
  • The Aurora kinases are a family of serine/threonine kinases that are key regulators of mitosis and cytokinesis. PF-03814735 is a reversible inhibitor of both Aurora A and B kinases with IC50 values of 0.8 and 5 nM, respectively, in in vitro activity assays.{22524} PF-03814735 also inhibits the kinases FLT1, FAK, TrkA, Met, and FGFR1 with IC50 values of 10, 22, 30, 100, and 100 nM, respectively.{22524} PF-03814735 inhibits cell proliferation of HCT116, HL-60, A549, and H125 tumor cell lines with IC50 values ranging from 42-150 nM and shows in vivo efficacy in an HCT116 tumor xenograft mouse model.{22524} PF-03814735 has been shown to be particularly sensitive towards inhibiting the growth of small cell lung cancer cell lines and other tumors driven by the Myc family genes.{22525}  

     

    Brand:
    Cayman
    SKU:-
  • The Aurora kinases are a family of serine/threonine kinases that are key regulators of mitosis and cytokinesis. PF-03814735 is a reversible inhibitor of both Aurora A and B kinases with IC50 values of 0.8 and 5 nM, respectively, in in vitro activity assays.{22524} PF-03814735 also inhibits the kinases FLT1, FAK, TrkA, Met, and FGFR1 with IC50 values of 10, 22, 30, 100, and 100 nM, respectively.{22524} PF-03814735 inhibits cell proliferation of HCT116, HL-60, A549, and H125 tumor cell lines with IC50 values ranging from 42-150 nM and shows in vivo efficacy in an HCT116 tumor xenograft mouse model.{22524} PF-03814735 has been shown to be particularly sensitive towards inhibiting the growth of small cell lung cancer cell lines and other tumors driven by the Myc family genes.{22525}  

     

    Brand:
    Cayman
    SKU:-
  • The Aurora kinases are a family of serine/threonine kinases that are key regulators of mitosis and cytokinesis. PF-03814735 is a reversible inhibitor of both Aurora A and B kinases with IC50 values of 0.8 and 5 nM, respectively, in in vitro activity assays.{22524} PF-03814735 also inhibits the kinases FLT1, FAK, TrkA, Met, and FGFR1 with IC50 values of 10, 22, 30, 100, and 100 nM, respectively.{22524} PF-03814735 inhibits cell proliferation of HCT116, HL-60, A549, and H125 tumor cell lines with IC50 values ranging from 42-150 nM and shows in vivo efficacy in an HCT116 tumor xenograft mouse model.{22524} PF-03814735 has been shown to be particularly sensitive towards inhibiting the growth of small cell lung cancer cell lines and other tumors driven by the Myc family genes.{22525}  

     

    Brand:
    Cayman
    SKU:-
  • The Aurora kinases are a family of serine/threonine kinases that are key regulators of mitosis and cytokinesis. PF-03814735 is a reversible inhibitor of both Aurora A and B kinases with IC50 values of 0.8 and 5 nM, respectively, in in vitro activity assays.{22524} PF-03814735 also inhibits the kinases FLT1, FAK, TrkA, Met, and FGFR1 with IC50 values of 10, 22, 30, 100, and 100 nM, respectively.{22524} PF-03814735 inhibits cell proliferation of HCT116, HL-60, A549, and H125 tumor cell lines with IC50 values ranging from 42-150 nM and shows in vivo efficacy in an HCT116 tumor xenograft mouse model.{22524} PF-03814735 has been shown to be particularly sensitive towards inhibiting the growth of small cell lung cancer cell lines and other tumors driven by the Myc family genes.{22525}  

     

    Brand:
    Cayman
    SKU:-
  • MET is a proto-oncogene that encodes the hepatocyte growth factor receptor c-Met. It has normal roles in morphogenesis, migration, apoptosis, and angiogenesis. Dysregulation of c-Met occurs in many types of cancer. PF-04217903 is a class I c-Met kinase inhibitor (Ki = 4.8 nM) that demonstrates more than 1,000-fold selectivity for c-Met compared with more than 150 kinases.{29778} It can inhibit tumor cell proliferation, survival, and migration/invasion in MET-amplified cell lines in vitro (IC50s = 12-31 nM), and shows antitumor activity in in vivo tumor models harboring either MET gene amplification or a hepatocyte growth factor/c-Met autocrine loop.{29778} PF-04217903 underwent phase I clinical trials in 2010.{23657}  

     

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    Cayman
    SKU:-

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  • MET is a proto-oncogene that encodes the hepatocyte growth factor receptor c-Met. It has normal roles in morphogenesis, migration, apoptosis, and angiogenesis. Dysregulation of c-Met occurs in many types of cancer. PF-04217903 is a class I c-Met kinase inhibitor (Ki = 4.8 nM) that demonstrates more than 1,000-fold selectivity for c-Met compared with more than 150 kinases.{29778} It can inhibit tumor cell proliferation, survival, and migration/invasion in MET-amplified cell lines in vitro (IC50s = 12-31 nM), and shows antitumor activity in in vivo tumor models harboring either MET gene amplification or a hepatocyte growth factor/c-Met autocrine loop.{29778} PF-04217903 underwent phase I clinical trials in 2010.{23657}  

     

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    Cayman
    SKU:-

    Available on backorder

  • MET is a proto-oncogene that encodes the hepatocyte growth factor receptor c-Met. It has normal roles in morphogenesis, migration, apoptosis, and angiogenesis. Dysregulation of c-Met occurs in many types of cancer. PF-04217903 is a class I c-Met kinase inhibitor (Ki = 4.8 nM) that demonstrates more than 1,000-fold selectivity for c-Met compared with more than 150 kinases.{29778} It can inhibit tumor cell proliferation, survival, and migration/invasion in MET-amplified cell lines in vitro (IC50s = 12-31 nM), and shows antitumor activity in in vivo tumor models harboring either MET gene amplification or a hepatocyte growth factor/c-Met autocrine loop.{29778} PF-04217903 underwent phase I clinical trials in 2010.{23657}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • MET is a proto-oncogene that encodes the hepatocyte growth factor receptor c-Met. It has normal roles in morphogenesis, migration, apoptosis, and angiogenesis. Dysregulation of c-Met occurs in many types of cancer. PF-04217903 is a class I c-Met kinase inhibitor (Ki = 4.8 nM) that demonstrates more than 1,000-fold selectivity for c-Met compared with more than 150 kinases.{29778} It can inhibit tumor cell proliferation, survival, and migration/invasion in MET-amplified cell lines in vitro (IC50s = 12-31 nM), and shows antitumor activity in in vivo tumor models harboring either MET gene amplification or a hepatocyte growth factor/c-Met autocrine loop.{29778} PF-04217903 underwent phase I clinical trials in 2010.{23657}  

     

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    Cayman
    SKU:-

    Available on backorder

  • Prostaglandin E2 (PGE2) evokes distinct responses through four different ‘E prostanoid’ (EP) receptors. EP2 is a G protein-coupled receptor which signals preferentially through Gs proteins. PF-04418948 is an orally active, potent, and selective EP2 receptor antagonist (IC50 = 16 nM).{22584} It is over a thousand-fold less active at other prostanoid receptors, including other EP receptors. PF-04418948 can be used in cells and tissues.{22583,22585} In rats, it significantly reduces the effects of the EP2-selective agonist butaprost on cutaneous blood flow when given orally.{22584}  

     

    Brand:
    Cayman
    SKU:-
  • Prostaglandin E2 (PGE2) evokes distinct responses through four different ‘E prostanoid’ (EP) receptors. EP2 is a G protein-coupled receptor which signals preferentially through Gs proteins. PF-04418948 is an orally active, potent, and selective EP2 receptor antagonist (IC50 = 16 nM).{22584} It is over a thousand-fold less active at other prostanoid receptors, including other EP receptors. PF-04418948 can be used in cells and tissues.{22583,22585} In rats, it significantly reduces the effects of the EP2-selective agonist butaprost on cutaneous blood flow when given orally.{22584}  

     

    Brand:
    Cayman
    SKU:-
  • Prostaglandin E2 (PGE2) evokes distinct responses through four different ‘E prostanoid’ (EP) receptors. EP2 is a G protein-coupled receptor which signals preferentially through Gs proteins. PF-04418948 is an orally active, potent, and selective EP2 receptor antagonist (IC50 = 16 nM).{22584} It is over a thousand-fold less active at other prostanoid receptors, including other EP receptors. PF-04418948 can be used in cells and tissues.{22583,22585} In rats, it significantly reduces the effects of the EP2-selective agonist butaprost on cutaneous blood flow when given orally.{22584}  

     

    Brand:
    Cayman
    SKU:-
  • Prostaglandin E2 (PGE2) evokes distinct responses through four different ‘E prostanoid’ (EP) receptors. EP2 is a G protein-coupled receptor which signals preferentially through Gs proteins. PF-04418948 is an orally active, potent, and selective EP2 receptor antagonist (IC50 = 16 nM).{22584} It is over a thousand-fold less active at other prostanoid receptors, including other EP receptors. PF-04418948 can be used in cells and tissues.{22583,22585} In rats, it significantly reduces the effects of the EP2-selective agonist butaprost on cutaneous blood flow when given orally.{22584}  

     

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    Cayman
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  • PF-04447943 is a brain-permeable phosphodiesterase (PDE) inhibitor that is selective for PDE9A (IC50 = 12 nM) over other PDEs (IC50s = >940 nM) in enzymatic assays of second messenger hydrolysis.{41434} It is over 1,000-fold more selective for PDE9A over 79 non-PDE targets, with the exception of the melatonin MT3/ML2 receptor (Ki = 3,800 nM). PF-04447943 also inhibits rat and rhesus monkey PDE9A (Kis = 18.1 and 4.5 nM, respectively).{41435} It increases neurite outgrowth and the density of synapsin puncta in primary rat hippocampal neurons when used at a concentration of 0.03 μM. PF-04447943 increases the cGMP level in the striatum and frontal cortex of mice and in the cerebrospinal fluid (CSF) of rats when administered at 10 and 1 mg/kg, respectively.{41434} It improves deficits in episodic memory induced by scopolamine (Item No. 14108) in rats and increases the time spent exploring the novel object in the novel object recognition (NOR) test when administered at a dose of 1 mg/kg. PF-04447943 (3.2 mg/kg) also improves spatial memory in the Morris water maze (MWM) and decreases the distance traveled to the hidden platform.  

     

    Brand:
    Cayman
    SKU:24299 - 1 mg

    Available on backorder

  • PF-04447943 is a brain-permeable phosphodiesterase (PDE) inhibitor that is selective for PDE9A (IC50 = 12 nM) over other PDEs (IC50s = >940 nM) in enzymatic assays of second messenger hydrolysis.{41434} It is over 1,000-fold more selective for PDE9A over 79 non-PDE targets, with the exception of the melatonin MT3/ML2 receptor (Ki = 3,800 nM). PF-04447943 also inhibits rat and rhesus monkey PDE9A (Kis = 18.1 and 4.5 nM, respectively).{41435} It increases neurite outgrowth and the density of synapsin puncta in primary rat hippocampal neurons when used at a concentration of 0.03 μM. PF-04447943 increases the cGMP level in the striatum and frontal cortex of mice and in the cerebrospinal fluid (CSF) of rats when administered at 10 and 1 mg/kg, respectively.{41434} It improves deficits in episodic memory induced by scopolamine (Item No. 14108) in rats and increases the time spent exploring the novel object in the novel object recognition (NOR) test when administered at a dose of 1 mg/kg. PF-04447943 (3.2 mg/kg) also improves spatial memory in the Morris water maze (MWM) and decreases the distance traveled to the hidden platform.  

     

    Brand:
    Cayman
    SKU:24299 - 10 mg

    Available on backorder

  • PF-04447943 is a brain-permeable phosphodiesterase (PDE) inhibitor that is selective for PDE9A (IC50 = 12 nM) over other PDEs (IC50s = >940 nM) in enzymatic assays of second messenger hydrolysis.{41434} It is over 1,000-fold more selective for PDE9A over 79 non-PDE targets, with the exception of the melatonin MT3/ML2 receptor (Ki = 3,800 nM). PF-04447943 also inhibits rat and rhesus monkey PDE9A (Kis = 18.1 and 4.5 nM, respectively).{41435} It increases neurite outgrowth and the density of synapsin puncta in primary rat hippocampal neurons when used at a concentration of 0.03 μM. PF-04447943 increases the cGMP level in the striatum and frontal cortex of mice and in the cerebrospinal fluid (CSF) of rats when administered at 10 and 1 mg/kg, respectively.{41434} It improves deficits in episodic memory induced by scopolamine (Item No. 14108) in rats and increases the time spent exploring the novel object in the novel object recognition (NOR) test when administered at a dose of 1 mg/kg. PF-04447943 (3.2 mg/kg) also improves spatial memory in the Morris water maze (MWM) and decreases the distance traveled to the hidden platform.  

     

    Brand:
    Cayman
    SKU:24299 - 25 mg

    Available on backorder

  • PF-04447943 is a brain-permeable phosphodiesterase (PDE) inhibitor that is selective for PDE9A (IC50 = 12 nM) over other PDEs (IC50s = >940 nM) in enzymatic assays of second messenger hydrolysis.{41434} It is over 1,000-fold more selective for PDE9A over 79 non-PDE targets, with the exception of the melatonin MT3/ML2 receptor (Ki = 3,800 nM). PF-04447943 also inhibits rat and rhesus monkey PDE9A (Kis = 18.1 and 4.5 nM, respectively).{41435} It increases neurite outgrowth and the density of synapsin puncta in primary rat hippocampal neurons when used at a concentration of 0.03 μM. PF-04447943 increases the cGMP level in the striatum and frontal cortex of mice and in the cerebrospinal fluid (CSF) of rats when administered at 10 and 1 mg/kg, respectively.{41434} It improves deficits in episodic memory induced by scopolamine (Item No. 14108) in rats and increases the time spent exploring the novel object in the novel object recognition (NOR) test when administered at a dose of 1 mg/kg. PF-04447943 (3.2 mg/kg) also improves spatial memory in the Morris water maze (MWM) and decreases the distance traveled to the hidden platform.  

     

    Brand:
    Cayman
    SKU:24299 - 5 mg

    Available on backorder

  • PF-04449613 is a phosphodiesterase 9A (PDE9A) inhibitor (IC50 = 22 nM).{54234} It is selective for PDE9A over PDE1C (IC50 = >1,000 nM), as well as over a variety of other PDEs, inhibiting PDE2-8, -10, and -11 activity by less than 30% in a panel of enzymes, ion channels, and transporters at 1 µM but does inhibit the human dopamine transporter (DAT; Ki = 293 nM). PF-04449613 (0.1-100 mg/kg, s.c.) increases cerebrospinal fluid (CSF) levels of cyclic GMP (cGMP) in rats. Subcutaneous administration of PF-04449613 (10 mg/kg) increases the rate of dendritic spine formation and elimination in mouse primary motor cortex pyramidal neurons in vivo.{54235} It increases the average running speed of mice in an accelerating rotarod task, indicating improved motor learning, at the same dose.  

     

    Brand:
    Cayman
    SKU:30946 - 1 mg

    Available on backorder

  • PF-04449613 is a phosphodiesterase 9A (PDE9A) inhibitor (IC50 = 22 nM).{54234} It is selective for PDE9A over PDE1C (IC50 = >1,000 nM), as well as over a variety of other PDEs, inhibiting PDE2-8, -10, and -11 activity by less than 30% in a panel of enzymes, ion channels, and transporters at 1 µM but does inhibit the human dopamine transporter (DAT; Ki = 293 nM). PF-04449613 (0.1-100 mg/kg, s.c.) increases cerebrospinal fluid (CSF) levels of cyclic GMP (cGMP) in rats. Subcutaneous administration of PF-04449613 (10 mg/kg) increases the rate of dendritic spine formation and elimination in mouse primary motor cortex pyramidal neurons in vivo.{54235} It increases the average running speed of mice in an accelerating rotarod task, indicating improved motor learning, at the same dose.  

     

    Brand:
    Cayman
    SKU:30946 - 10 mg

    Available on backorder

  • PF-04449613 is a phosphodiesterase 9A (PDE9A) inhibitor (IC50 = 22 nM).{54234} It is selective for PDE9A over PDE1C (IC50 = >1,000 nM), as well as over a variety of other PDEs, inhibiting PDE2-8, -10, and -11 activity by less than 30% in a panel of enzymes, ion channels, and transporters at 1 µM but does inhibit the human dopamine transporter (DAT; Ki = 293 nM). PF-04449613 (0.1-100 mg/kg, s.c.) increases cerebrospinal fluid (CSF) levels of cyclic GMP (cGMP) in rats. Subcutaneous administration of PF-04449613 (10 mg/kg) increases the rate of dendritic spine formation and elimination in mouse primary motor cortex pyramidal neurons in vivo.{54235} It increases the average running speed of mice in an accelerating rotarod task, indicating improved motor learning, at the same dose.  

     

    Brand:
    Cayman
    SKU:30946 - 25 mg

    Available on backorder

  • PF-04449613 is a phosphodiesterase 9A (PDE9A) inhibitor (IC50 = 22 nM).{54234} It is selective for PDE9A over PDE1C (IC50 = >1,000 nM), as well as over a variety of other PDEs, inhibiting PDE2-8, -10, and -11 activity by less than 30% in a panel of enzymes, ion channels, and transporters at 1 µM but does inhibit the human dopamine transporter (DAT; Ki = 293 nM). PF-04449613 (0.1-100 mg/kg, s.c.) increases cerebrospinal fluid (CSF) levels of cyclic GMP (cGMP) in rats. Subcutaneous administration of PF-04449613 (10 mg/kg) increases the rate of dendritic spine formation and elimination in mouse primary motor cortex pyramidal neurons in vivo.{54235} It increases the average running speed of mice in an accelerating rotarod task, indicating improved motor learning, at the same dose.  

     

    Brand:
    Cayman
    SKU:30946 - 5 mg

    Available on backorder

  • PF-04449913 is an orally available Hedgehog pathway inhibitor that acts by binding Smoothened (Smo) and blocking signal transduction (IC50 = 5 nM).{33585} It has been shown to attenuate leukemia stem cell self-renewal and cell cycle progression in primary acute myeloid leukemia cells and in an in vivo Drosophila model.{33586,33584}  

     

    Brand:
    Cayman
    SKU:9002936 - 1 mg

    Available on backorder

  • PF-04449913 is an orally available Hedgehog pathway inhibitor that acts by binding Smoothened (Smo) and blocking signal transduction (IC50 = 5 nM).{33585} It has been shown to attenuate leukemia stem cell self-renewal and cell cycle progression in primary acute myeloid leukemia cells and in an in vivo Drosophila model.{33586,33584}  

     

    Brand:
    Cayman
    SKU:9002936 - 10 mg

    Available on backorder

  • PF-04449913 is an orally available Hedgehog pathway inhibitor that acts by binding Smoothened (Smo) and blocking signal transduction (IC50 = 5 nM).{33585} It has been shown to attenuate leukemia stem cell self-renewal and cell cycle progression in primary acute myeloid leukemia cells and in an in vivo Drosophila model.{33586,33584}  

     

    Brand:
    Cayman
    SKU:9002936 - 25 mg

    Available on backorder

  • PF-04449913 is an orally available Hedgehog pathway inhibitor that acts by binding Smoothened (Smo) and blocking signal transduction (IC50 = 5 nM).{33585} It has been shown to attenuate leukemia stem cell self-renewal and cell cycle progression in primary acute myeloid leukemia cells and in an in vivo Drosophila model.{33586,33584}  

     

    Brand:
    Cayman
    SKU:9002936 - 5 mg

    Available on backorder

  • PF-04457845 is an orally active, irreversible inhibitor of fatty acid amide hydrolase (FAAH; IC50 = 7.2 nM) that is selective against other serine hydrolases.{20459} It is a covalent inhibitor that carbamylates the active site serine nucleophile of FAAH.{20459} In a rat model of inflammatory pain, oral administration of 0.1 mg/kg PF-04457845 has been shown to reduce inflammatory pain with efficacy comparable to that of naproxen.{20459}  

     

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    Cayman
    SKU:-

    Available on backorder

  • PF-04457845 is an orally active, irreversible inhibitor of fatty acid amide hydrolase (FAAH; IC50 = 7.2 nM) that is selective against other serine hydrolases.{20459} It is a covalent inhibitor that carbamylates the active site serine nucleophile of FAAH.{20459} In a rat model of inflammatory pain, oral administration of 0.1 mg/kg PF-04457845 has been shown to reduce inflammatory pain with efficacy comparable to that of naproxen.{20459}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • PF-04457845 is an orally active, irreversible inhibitor of fatty acid amide hydrolase (FAAH; IC50 = 7.2 nM) that is selective against other serine hydrolases.{20459} It is a covalent inhibitor that carbamylates the active site serine nucleophile of FAAH.{20459} In a rat model of inflammatory pain, oral administration of 0.1 mg/kg PF-04457845 has been shown to reduce inflammatory pain with efficacy comparable to that of naproxen.{20459}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • PF-04457845 is an orally active, irreversible inhibitor of fatty acid amide hydrolase (FAAH; IC50 = 7.2 nM) that is selective against other serine hydrolases.{20459} It is a covalent inhibitor that carbamylates the active site serine nucleophile of FAAH.{20459} In a rat model of inflammatory pain, oral administration of 0.1 mg/kg PF-04457845 has been shown to reduce inflammatory pain with efficacy comparable to that of naproxen.{20459}  

     

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    Cayman
    SKU:-

    Available on backorder

  • Acyl-CoA:diacylglycerol acyltransferase-1 (DGAT-1) catalyzes the final committed step in the biosynthesis of triglycerides and has potential roles in obesity, diabetes, and atherosclerosis.{12021,15816,10960} PF-04620110 is a potent inhibitor of DGAT-1 (IC50 = 19 nM) that is without effect on DGAT-2.{26854} It has high oral bioavailability (100%) in rats, with a moderate half-life of 6.8 hours.{26854} PF-04620110 significantly blocks an increase in plasma triglyceride levels following a corn oil bolus in rats.{26854}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • Acyl-CoA:diacylglycerol acyltransferase-1 (DGAT-1) catalyzes the final committed step in the biosynthesis of triglycerides and has potential roles in obesity, diabetes, and atherosclerosis.{12021,15816,10960} PF-04620110 is a potent inhibitor of DGAT-1 (IC50 = 19 nM) that is without effect on DGAT-2.{26854} It has high oral bioavailability (100%) in rats, with a moderate half-life of 6.8 hours.{26854} PF-04620110 significantly blocks an increase in plasma triglyceride levels following a corn oil bolus in rats.{26854}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • Acyl-CoA:diacylglycerol acyltransferase-1 (DGAT-1) catalyzes the final committed step in the biosynthesis of triglycerides and has potential roles in obesity, diabetes, and atherosclerosis.{12021,15816,10960} PF-04620110 is a potent inhibitor of DGAT-1 (IC50 = 19 nM) that is without effect on DGAT-2.{26854} It has high oral bioavailability (100%) in rats, with a moderate half-life of 6.8 hours.{26854} PF-04620110 significantly blocks an increase in plasma triglyceride levels following a corn oil bolus in rats.{26854}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • P70 ribosomal S6 kinase (S6K1) is a serine/threonine kinase which is activated by insulin and growth factors through PI3K and mTORC1 signaling pathways. PF-04708671 is a specific, cell-permeable inhibitor of S6K1 (IC50 = 160 nM).{22617} It does not inhibit S6K2, MSK, or RSK, or many other unrelated kinases, under conditions in which it inhibits S6K1 activity.{22617} It is useful in evaluating the role of S6K1 and, indirectly, mTORC1, in cell signaling.{22618,22616}  

     

    Brand:
    Cayman
    SKU:-
  • P70 ribosomal S6 kinase (S6K1) is a serine/threonine kinase which is activated by insulin and growth factors through PI3K and mTORC1 signaling pathways. PF-04708671 is a specific, cell-permeable inhibitor of S6K1 (IC50 = 160 nM).{22617} It does not inhibit S6K2, MSK, or RSK, or many other unrelated kinases, under conditions in which it inhibits S6K1 activity.{22617} It is useful in evaluating the role of S6K1 and, indirectly, mTORC1, in cell signaling.{22618,22616}  

     

    Brand:
    Cayman
    SKU:-
  • P70 ribosomal S6 kinase (S6K1) is a serine/threonine kinase which is activated by insulin and growth factors through PI3K and mTORC1 signaling pathways. PF-04708671 is a specific, cell-permeable inhibitor of S6K1 (IC50 = 160 nM).{22617} It does not inhibit S6K2, MSK, or RSK, or many other unrelated kinases, under conditions in which it inhibits S6K1 activity.{22617} It is useful in evaluating the role of S6K1 and, indirectly, mTORC1, in cell signaling.{22618,22616}  

     

    Brand:
    Cayman
    SKU:-
  • P70 ribosomal S6 kinase (S6K1) is a serine/threonine kinase which is activated by insulin and growth factors through PI3K and mTORC1 signaling pathways. PF-04708671 is a specific, cell-permeable inhibitor of S6K1 (IC50 = 160 nM).{22617} It does not inhibit S6K2, MSK, or RSK, or many other unrelated kinases, under conditions in which it inhibits S6K1 activity.{22617} It is useful in evaluating the role of S6K1 and, indirectly, mTORC1, in cell signaling.{22618,22616}  

     

    Brand:
    Cayman
    SKU:-
  • PF-04859989 is an inhibitor of kynurenine aminotransferase II (KAT II; IC50s = 0.032 and 0.263 µM for human and rat recombinant enzymes, respectively).{59036} It is selective for KAT II over KAT I, -III, and -IV (IC50s = 21.6, 107, and >50 µM, respectively). In vivo, PF-04859989 (10 mg/kg, s.c.) reduces basal striatum, prefrontal cortex, and hippocampus kynurenic acid levels in rats. It prevents ketamine- or amphetamine-induced disruption of auditory gating in rats, as well as prevents ketamine-induced deficits in spatial memory in non-human primates. PF-04859989 also inhibits glutamate oxaloacetate transaminase 1 (GOT1; IC50 = 8 µM) and reduces the viability of PaTu 8988t and PaTu 8902 pancreatic cancer cells in a concentration-dependent manner.{59037}  

     

    Brand:
    Cayman
    SKU:31383 - 1 mg

    Available on backorder

  • PF-04859989 is an inhibitor of kynurenine aminotransferase II (KAT II; IC50s = 0.032 and 0.263 µM for human and rat recombinant enzymes, respectively).{59036} It is selective for KAT II over KAT I, -III, and -IV (IC50s = 21.6, 107, and >50 µM, respectively). In vivo, PF-04859989 (10 mg/kg, s.c.) reduces basal striatum, prefrontal cortex, and hippocampus kynurenic acid levels in rats. It prevents ketamine- or amphetamine-induced disruption of auditory gating in rats, as well as prevents ketamine-induced deficits in spatial memory in non-human primates. PF-04859989 also inhibits glutamate oxaloacetate transaminase 1 (GOT1; IC50 = 8 µM) and reduces the viability of PaTu 8988t and PaTu 8902 pancreatic cancer cells in a concentration-dependent manner.{59037}  

     

    Brand:
    Cayman
    SKU:31383 - 10 mg

    Available on backorder

  • PF-04859989 is an inhibitor of kynurenine aminotransferase II (KAT II; IC50s = 0.032 and 0.263 µM for human and rat recombinant enzymes, respectively).{59036} It is selective for KAT II over KAT I, -III, and -IV (IC50s = 21.6, 107, and >50 µM, respectively). In vivo, PF-04859989 (10 mg/kg, s.c.) reduces basal striatum, prefrontal cortex, and hippocampus kynurenic acid levels in rats. It prevents ketamine- or amphetamine-induced disruption of auditory gating in rats, as well as prevents ketamine-induced deficits in spatial memory in non-human primates. PF-04859989 also inhibits glutamate oxaloacetate transaminase 1 (GOT1; IC50 = 8 µM) and reduces the viability of PaTu 8988t and PaTu 8902 pancreatic cancer cells in a concentration-dependent manner.{59037}  

     

    Brand:
    Cayman
    SKU:31383 - 25 mg

    Available on backorder

  • PF-04859989 is an inhibitor of kynurenine aminotransferase II (KAT II; IC50s = 0.032 and 0.263 µM for human and rat recombinant enzymes, respectively).{59036} It is selective for KAT II over KAT I, -III, and -IV (IC50s = 21.6, 107, and >50 µM, respectively). In vivo, PF-04859989 (10 mg/kg, s.c.) reduces basal striatum, prefrontal cortex, and hippocampus kynurenic acid levels in rats. It prevents ketamine- or amphetamine-induced disruption of auditory gating in rats, as well as prevents ketamine-induced deficits in spatial memory in non-human primates. PF-04859989 also inhibits glutamate oxaloacetate transaminase 1 (GOT1; IC50 = 8 µM) and reduces the viability of PaTu 8988t and PaTu 8902 pancreatic cancer cells in a concentration-dependent manner.{59037}  

     

    Brand:
    Cayman
    SKU:31383 - 5 mg

    Available on backorder

  • PF-04929113 is a prodrug for the Hsp90 inhibitor, PF-04958473 (SNX-2112; Item No. 22359), which binds both Hsp90α and Hsp90β with an IC50 value of 30 nM.{31149,31150} The prodrug, PF-04929113, is rapidly absorbed and converted into the active inhibitor after oral administration.{31150} The active inhibitor causes degradation of Hsp90 client proteins, including HER2, and reduces phosphorylation of downstream kinases, including Akt and ERK1/2, leading to apoptosis in cancer cells.{31149,31152} Oral administration of the prodrug, PF-04929113, reduces tumor growth and prolongs survival in mouse models of multiple myeloma and prostate cancer.{31152,31151}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • PF-04929113 is a prodrug for the Hsp90 inhibitor, PF-04958473 (SNX-2112; Item No. 22359), which binds both Hsp90α and Hsp90β with an IC50 value of 30 nM.{31149,31150} The prodrug, PF-04929113, is rapidly absorbed and converted into the active inhibitor after oral administration.{31150} The active inhibitor causes degradation of Hsp90 client proteins, including HER2, and reduces phosphorylation of downstream kinases, including Akt and ERK1/2, leading to apoptosis in cancer cells.{31149,31152} Oral administration of the prodrug, PF-04929113, reduces tumor growth and prolongs survival in mouse models of multiple myeloma and prostate cancer.{31152,31151}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • PF-04929113 is a prodrug for the Hsp90 inhibitor, PF-04958473 (SNX-2112; Item No. 22359), which binds both Hsp90α and Hsp90β with an IC50 value of 30 nM.{31149,31150} The prodrug, PF-04929113, is rapidly absorbed and converted into the active inhibitor after oral administration.{31150} The active inhibitor causes degradation of Hsp90 client proteins, including HER2, and reduces phosphorylation of downstream kinases, including Akt and ERK1/2, leading to apoptosis in cancer cells.{31149,31152} Oral administration of the prodrug, PF-04929113, reduces tumor growth and prolongs survival in mouse models of multiple myeloma and prostate cancer.{31152,31151}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • PF-04929113 is a prodrug for the Hsp90 inhibitor, PF-04958473 (SNX-2112; Item No. 22359), which binds both Hsp90α and Hsp90β with an IC50 value of 30 nM.{31149,31150} The prodrug, PF-04929113, is rapidly absorbed and converted into the active inhibitor after oral administration.{31150} The active inhibitor causes degradation of Hsp90 client proteins, including HER2, and reduces phosphorylation of downstream kinases, including Akt and ERK1/2, leading to apoptosis in cancer cells.{31149,31152} Oral administration of the prodrug, PF-04929113, reduces tumor growth and prolongs survival in mouse models of multiple myeloma and prostate cancer.{31152,31151}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • PF-04981517 is a potent, time-dependent inhibitor of the cytochrome P450 (CYP450) isoform CYP3A4 (IC50 = 30 nM).{22614} It is less effective against CYP3A5 and CYP3A7 (IC50s = 17 and 70 μM, respectively).{22614} PF-04981517 will be useful for understanding the relative roles of CYP3A4 and CYP3A5 in drug metabolism.  

     

    Brand:
    Cayman
    SKU:-
  • PF-04981517 is a potent, time-dependent inhibitor of the cytochrome P450 (CYP450) isoform CYP3A4 (IC50 = 30 nM).{22614} It is less effective against CYP3A5 and CYP3A7 (IC50s = 17 and 70 μM, respectively).{22614} PF-04981517 will be useful for understanding the relative roles of CYP3A4 and CYP3A5 in drug metabolism.  

     

    Brand:
    Cayman
    SKU:-
  • PF-04981517 is a potent, time-dependent inhibitor of the cytochrome P450 (CYP450) isoform CYP3A4 (IC50 = 30 nM).{22614} It is less effective against CYP3A5 and CYP3A7 (IC50s = 17 and 70 μM, respectively).{22614} PF-04981517 will be useful for understanding the relative roles of CYP3A4 and CYP3A5 in drug metabolism.  

     

    Brand:
    Cayman
    SKU:-
  • PF-04981517 is a potent, time-dependent inhibitor of the cytochrome P450 (CYP450) isoform CYP3A4 (IC50 = 30 nM).{22614} It is less effective against CYP3A5 and CYP3A7 (IC50s = 17 and 70 μM, respectively).{22614} PF-04981517 will be useful for understanding the relative roles of CYP3A4 and CYP3A5 in drug metabolism.  

     

    Brand:
    Cayman
    SKU:-
  • PF-04995274 is a partial agonist of the serotonin (5-HT) receptor subtypes 5-HT4A, 5-HT4B, 5-HT4D, and 5-HT4E (Kis = 0.36, 0.46, 0.15, and 0.32 nM, respectively, in a radioligand binding assay).{52049} It increases cAMP levels in HEK293 cells expressing 5-HT4A, 5-HT4B, 5-HT4D, and 5-HT4E receptors (EC50s = 0.47, 0.36, 0.37, and 0.26 nM, respectively, for the human recombinant receptors). PF-04995274 decreases scopolamine-induced increases in the distance traveled in the Morris water maze in rats when administered at a dose of 0.032 mg/kg.  

     

    Brand:
    Cayman
    SKU:28776 - 1 mg

    Available on backorder

  • PF-04995274 is a partial agonist of the serotonin (5-HT) receptor subtypes 5-HT4A, 5-HT4B, 5-HT4D, and 5-HT4E (Kis = 0.36, 0.46, 0.15, and 0.32 nM, respectively, in a radioligand binding assay).{52049} It increases cAMP levels in HEK293 cells expressing 5-HT4A, 5-HT4B, 5-HT4D, and 5-HT4E receptors (EC50s = 0.47, 0.36, 0.37, and 0.26 nM, respectively, for the human recombinant receptors). PF-04995274 decreases scopolamine-induced increases in the distance traveled in the Morris water maze in rats when administered at a dose of 0.032 mg/kg.  

     

    Brand:
    Cayman
    SKU:28776 - 10 mg

    Available on backorder

  • PF-04995274 is a partial agonist of the serotonin (5-HT) receptor subtypes 5-HT4A, 5-HT4B, 5-HT4D, and 5-HT4E (Kis = 0.36, 0.46, 0.15, and 0.32 nM, respectively, in a radioligand binding assay).{52049} It increases cAMP levels in HEK293 cells expressing 5-HT4A, 5-HT4B, 5-HT4D, and 5-HT4E receptors (EC50s = 0.47, 0.36, 0.37, and 0.26 nM, respectively, for the human recombinant receptors). PF-04995274 decreases scopolamine-induced increases in the distance traveled in the Morris water maze in rats when administered at a dose of 0.032 mg/kg.  

     

    Brand:
    Cayman
    SKU:28776 - 25 mg

    Available on backorder

  • PF-04995274 is a partial agonist of the serotonin (5-HT) receptor subtypes 5-HT4A, 5-HT4B, 5-HT4D, and 5-HT4E (Kis = 0.36, 0.46, 0.15, and 0.32 nM, respectively, in a radioligand binding assay).{52049} It increases cAMP levels in HEK293 cells expressing 5-HT4A, 5-HT4B, 5-HT4D, and 5-HT4E receptors (EC50s = 0.47, 0.36, 0.37, and 0.26 nM, respectively, for the human recombinant receptors). PF-04995274 decreases scopolamine-induced increases in the distance traveled in the Morris water maze in rats when administered at a dose of 0.032 mg/kg.  

     

    Brand:
    Cayman
    SKU:28776 - 5 mg

    Available on backorder

  • PF-05089771 is a voltage-gated sodium channel 1.7 (Nav1.7) blocker (IC50s = 11, 16, 33, and 20 nM for 5N11S, 5A11L, 5A11S, and 5A11L Nav1.7 splice variants, respectively).{41748} It is selective for Nav1.7 over Nav1.1-1.6 and 1.8 channels (IC50s = 0.11-25 μM), L-type calcium, and KvLQT and hERG potassium channels (IC50s = ≥10 μM), as well as human and cynomolgus monkey TRPV1 receptors (IC50s = 10 and 20 μM, respectively). PF-05089771 is also 1,000-fold selective for half-inactivated over resting Nav1.7 channels, and mutation of the domain IV voltage-sensor domain (VSD4) reduces PF-05089771 potency by approximately 100-fold.  

     

    Brand:
    Cayman
    SKU:24449 - 10 mg

    Available on backorder

  • PF-05089771 is a voltage-gated sodium channel 1.7 (Nav1.7) blocker (IC50s = 11, 16, 33, and 20 nM for 5N11S, 5A11L, 5A11S, and 5A11L Nav1.7 splice variants, respectively).{41748} It is selective for Nav1.7 over Nav1.1-1.6 and 1.8 channels (IC50s = 0.11-25 μM), L-type calcium, and KvLQT and hERG potassium channels (IC50s = ≥10 μM), as well as human and cynomolgus monkey TRPV1 receptors (IC50s = 10 and 20 μM, respectively). PF-05089771 is also 1,000-fold selective for half-inactivated over resting Nav1.7 channels, and mutation of the domain IV voltage-sensor domain (VSD4) reduces PF-05089771 potency by approximately 100-fold.  

     

    Brand:
    Cayman
    SKU:24449 - 25 mg

    Available on backorder

  • PF-05089771 is a voltage-gated sodium channel 1.7 (Nav1.7) blocker (IC50s = 11, 16, 33, and 20 nM for 5N11S, 5A11L, 5A11S, and 5A11L Nav1.7 splice variants, respectively).{41748} It is selective for Nav1.7 over Nav1.1-1.6 and 1.8 channels (IC50s = 0.11-25 μM), L-type calcium, and KvLQT and hERG potassium channels (IC50s = ≥10 μM), as well as human and cynomolgus monkey TRPV1 receptors (IC50s = 10 and 20 μM, respectively). PF-05089771 is also 1,000-fold selective for half-inactivated over resting Nav1.7 channels, and mutation of the domain IV voltage-sensor domain (VSD4) reduces PF-05089771 potency by approximately 100-fold.  

     

    Brand:
    Cayman
    SKU:24449 - 5 mg

    Available on backorder

  • PF-05105679 is an antagonist of transient receptor potential melastatin 8 (TRPM8; IC50 = 103 nM for inhibition of voltage-activated currents in HEK293 cells expressing the human receptor).{52271} It is greater than 100-fold selective for TRPM8 over a panel of 90 receptors, ion channels, and enzymes. PF-05105679 inhibits calcium flux induced by cold or the TRPM8 agonist WS-12 in HEK293 cells expressing the human TRPM8 (IC50s = 480 and 181 nM, respectively). Intravenous infusion of PF-05105679 (46.67 μg/kg per minute) reverses cold-induced reductions in bladder capacity in anesthetized guinea pigs. It decreases the core body temperature in rats when administered at doses of 100 and 300 mg/kg.  

     

    Brand:
    Cayman
    SKU:29489 - 1 mg

    Available on backorder

  • PF-05105679 is an antagonist of transient receptor potential melastatin 8 (TRPM8; IC50 = 103 nM for inhibition of voltage-activated currents in HEK293 cells expressing the human receptor).{52271} It is greater than 100-fold selective for TRPM8 over a panel of 90 receptors, ion channels, and enzymes. PF-05105679 inhibits calcium flux induced by cold or the TRPM8 agonist WS-12 in HEK293 cells expressing the human TRPM8 (IC50s = 480 and 181 nM, respectively). Intravenous infusion of PF-05105679 (46.67 μg/kg per minute) reverses cold-induced reductions in bladder capacity in anesthetized guinea pigs. It decreases the core body temperature in rats when administered at doses of 100 and 300 mg/kg.  

     

    Brand:
    Cayman
    SKU:29489 - 10 mg

    Available on backorder

  • PF-05105679 is an antagonist of transient receptor potential melastatin 8 (TRPM8; IC50 = 103 nM for inhibition of voltage-activated currents in HEK293 cells expressing the human receptor).{52271} It is greater than 100-fold selective for TRPM8 over a panel of 90 receptors, ion channels, and enzymes. PF-05105679 inhibits calcium flux induced by cold or the TRPM8 agonist WS-12 in HEK293 cells expressing the human TRPM8 (IC50s = 480 and 181 nM, respectively). Intravenous infusion of PF-05105679 (46.67 μg/kg per minute) reverses cold-induced reductions in bladder capacity in anesthetized guinea pigs. It decreases the core body temperature in rats when administered at doses of 100 and 300 mg/kg.  

     

    Brand:
    Cayman
    SKU:29489 - 5 mg

    Available on backorder

  • PF-05175157 is an inhibitor of acetyl-CoA carboxylase 1 (ACC1) and ACC2 (IC50s = 27, 33, 23.5, and 50.4 nM for human ACC1, human ACC2, rat ACC1, and rat ACC2, respectively).{41717} It inhibits formation of malonyl-CoA in primary rat hepatocytes (EC50 = 29.9 nM). In vivo, PF-05175157 inhibits formation of malonyl-CoA in the liver and skeletal muscle, inhibits hepatic de novo lipogenesis, and lowers the respiratory exchange rate in rats (ED50s = 6, 11, 7.8, and 3.5 mg/kg, respectively).  

     

    Brand:
    Cayman
    SKU:21778 -

    Out of stock

  • PF-05175157 is an inhibitor of acetyl-CoA carboxylase 1 (ACC1) and ACC2 (IC50s = 27, 33, 23.5, and 50.4 nM for human ACC1, human ACC2, rat ACC1, and rat ACC2, respectively).{41717} It inhibits formation of malonyl-CoA in primary rat hepatocytes (EC50 = 29.9 nM). In vivo, PF-05175157 inhibits formation of malonyl-CoA in the liver and skeletal muscle, inhibits hepatic de novo lipogenesis, and lowers the respiratory exchange rate in rats (ED50s = 6, 11, 7.8, and 3.5 mg/kg, respectively).  

     

    Brand:
    Cayman
    SKU:21778 -

    Out of stock

  • PF-05175157 is an inhibitor of acetyl-CoA carboxylase 1 (ACC1) and ACC2 (IC50s = 27, 33, 23.5, and 50.4 nM for human ACC1, human ACC2, rat ACC1, and rat ACC2, respectively).{41717} It inhibits formation of malonyl-CoA in primary rat hepatocytes (EC50 = 29.9 nM). In vivo, PF-05175157 inhibits formation of malonyl-CoA in the liver and skeletal muscle, inhibits hepatic de novo lipogenesis, and lowers the respiratory exchange rate in rats (ED50s = 6, 11, 7.8, and 3.5 mg/kg, respectively).  

     

    Brand:
    Cayman
    SKU:21778 -

    Out of stock

  • PF-05175157 is an inhibitor of acetyl-CoA carboxylase 1 (ACC1) and ACC2 (IC50s = 27, 33, 23.5, and 50.4 nM for human ACC1, human ACC2, rat ACC1, and rat ACC2, respectively).{41717} It inhibits formation of malonyl-CoA in primary rat hepatocytes (EC50 = 29.9 nM). In vivo, PF-05175157 inhibits formation of malonyl-CoA in the liver and skeletal muscle, inhibits hepatic de novo lipogenesis, and lowers the respiratory exchange rate in rats (ED50s = 6, 11, 7.8, and 3.5 mg/kg, respectively).  

     

    Brand:
    Cayman
    SKU:21778 -

    Out of stock

  • PF-05180999 is a phosphodiesterase 2A (PDE2A) inhibitor (IC50 = 1.6 nM).{54068} It is greater than 2000-fold selective for PDE2A over a panel of ten additional PDEs. PF-05180999 increases striatal, cortical, and hippocampal cGMP levels in mice in a dose-dependent manner. In vivo, it inhibits disruption of low frequency cortical δ oscillation induced by the NMDA antagonist MK-801 in rat brain when administered at a dose of 0.03 mg/kg. PF-05180999 (0.1 and 0.32 mg/kg) inhibits ketamine-induced increases in the number of working memory errors in a radial arm maze task in rats.  

     

    Brand:
    Cayman
    SKU:30374 - 1 mg

    Available on backorder

  • PF-05180999 is a phosphodiesterase 2A (PDE2A) inhibitor (IC50 = 1.6 nM).{54068} It is greater than 2000-fold selective for PDE2A over a panel of ten additional PDEs. PF-05180999 increases striatal, cortical, and hippocampal cGMP levels in mice in a dose-dependent manner. In vivo, it inhibits disruption of low frequency cortical δ oscillation induced by the NMDA antagonist MK-801 in rat brain when administered at a dose of 0.03 mg/kg. PF-05180999 (0.1 and 0.32 mg/kg) inhibits ketamine-induced increases in the number of working memory errors in a radial arm maze task in rats.  

     

    Brand:
    Cayman
    SKU:30374 - 10 mg

    Available on backorder

  • PF-05180999 is a phosphodiesterase 2A (PDE2A) inhibitor (IC50 = 1.6 nM).{54068} It is greater than 2000-fold selective for PDE2A over a panel of ten additional PDEs. PF-05180999 increases striatal, cortical, and hippocampal cGMP levels in mice in a dose-dependent manner. In vivo, it inhibits disruption of low frequency cortical δ oscillation induced by the NMDA antagonist MK-801 in rat brain when administered at a dose of 0.03 mg/kg. PF-05180999 (0.1 and 0.32 mg/kg) inhibits ketamine-induced increases in the number of working memory errors in a radial arm maze task in rats.  

     

    Brand:
    Cayman
    SKU:30374 - 5 mg

    Available on backorder

  • Phosphatidylinositol-3-kinases (PI3Ks) act in concert with mTOR complexes to regulate signaling pathways that have critical roles in cancer and other diseases.{15415,27164} PF-05212384 is a potent, dual PI3K/mTOR inhibitor (IC50 values are 0.4 and 5.4 nM for PI3Kα and PI3Kγ, respectively, and 1.6 nM for mTOR).{29095,29096} It is active both in vitro and in vivo, inhibiting the growth of cancer cells in culture or in xenografts in mice when delivered intravenously.{29095,29096} PF-05212384 blocks the proliferation of liver cancer stem cells, and this effect is enhanced in combination therapy with the multikinase inhibitor BAY-43-9006 (Item No. 10009644).{29089} PF-05212384 action also enhances the effectiveness of cetuximab or radiation therapy in human head and neck cancer models.{29088,29094}  

     

    Brand:
    Cayman
    SKU:-
  • Phosphatidylinositol-3-kinases (PI3Ks) act in concert with mTOR complexes to regulate signaling pathways that have critical roles in cancer and other diseases.{15415,27164} PF-05212384 is a potent, dual PI3K/mTOR inhibitor (IC50 values are 0.4 and 5.4 nM for PI3Kα and PI3Kγ, respectively, and 1.6 nM for mTOR).{29095,29096} It is active both in vitro and in vivo, inhibiting the growth of cancer cells in culture or in xenografts in mice when delivered intravenously.{29095,29096} PF-05212384 blocks the proliferation of liver cancer stem cells, and this effect is enhanced in combination therapy with the multikinase inhibitor BAY-43-9006 (Item No. 10009644).{29089} PF-05212384 action also enhances the effectiveness of cetuximab or radiation therapy in human head and neck cancer models.{29088,29094}  

     

    Brand:
    Cayman
    SKU:-
  • Phosphatidylinositol-3-kinases (PI3Ks) act in concert with mTOR complexes to regulate signaling pathways that have critical roles in cancer and other diseases.{15415,27164} PF-05212384 is a potent, dual PI3K/mTOR inhibitor (IC50 values are 0.4 and 5.4 nM for PI3Kα and PI3Kγ, respectively, and 1.6 nM for mTOR).{29095,29096} It is active both in vitro and in vivo, inhibiting the growth of cancer cells in culture or in xenografts in mice when delivered intravenously.{29095,29096} PF-05212384 blocks the proliferation of liver cancer stem cells, and this effect is enhanced in combination therapy with the multikinase inhibitor BAY-43-9006 (Item No. 10009644).{29089} PF-05212384 action also enhances the effectiveness of cetuximab or radiation therapy in human head and neck cancer models.{29088,29094}  

     

    Brand:
    Cayman
    SKU:-