Cayman
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Eledoisin is an undecapeptide tachykinin neuropeptide and neurokinin (NK) receptor agonist originally isolated from E. moschata.{46470,46472} It binds to NK1 (pD2 = 9.5 and 9.21 in isolated dog carotid artery and guinea pig ileum, respectively), NK2 (pD2 = 8.22 and 7.7 in isolated rabbit pulmonary artery and rat duodenum, respectively), and NK3 receptors (pD2 = 7.11 and 7.06 in isolated rat portal vein and hamster urinary bladder, respectively).{46471} Eledoisin induces contraction of isolated guinea pig ileum and rabbit jejunum.{41381} It also induces salivation in rats and lowers arterial blood pressure in rabbits and guinea pigs in vivo.{41381,46473}
Brand:CaymanSKU:28810 - 1 mgAvailable on backorder
Eledoisin is an undecapeptide tachykinin neuropeptide and neurokinin (NK) receptor agonist originally isolated from E. moschata.{46470,46472} It binds to NK1 (pD2 = 9.5 and 9.21 in isolated dog carotid artery and guinea pig ileum, respectively), NK2 (pD2 = 8.22 and 7.7 in isolated rabbit pulmonary artery and rat duodenum, respectively), and NK3 receptors (pD2 = 7.11 and 7.06 in isolated rat portal vein and hamster urinary bladder, respectively).{46471} Eledoisin induces contraction of isolated guinea pig ileum and rabbit jejunum.{41381} It also induces salivation in rats and lowers arterial blood pressure in rabbits and guinea pigs in vivo.{41381,46473}
Brand:CaymanSKU:28810 - 10 mgAvailable on backorder
Eledoisin is an undecapeptide tachykinin neuropeptide and neurokinin (NK) receptor agonist originally isolated from E. moschata.{46470,46472} It binds to NK1 (pD2 = 9.5 and 9.21 in isolated dog carotid artery and guinea pig ileum, respectively), NK2 (pD2 = 8.22 and 7.7 in isolated rabbit pulmonary artery and rat duodenum, respectively), and NK3 receptors (pD2 = 7.11 and 7.06 in isolated rat portal vein and hamster urinary bladder, respectively).{46471} Eledoisin induces contraction of isolated guinea pig ileum and rabbit jejunum.{41381} It also induces salivation in rats and lowers arterial blood pressure in rabbits and guinea pigs in vivo.{41381,46473}
Brand:CaymanSKU:28810 - 5 mgAvailable on backorder
Elemicin is a trioxygenated phenylpropane that has been found in A. dracunculus.{49622} It is active against S. aureus, B. subtilis, and C. albicans (MICs = 600, 2,500, and 1,000 mg/L, respectively) but not E. coli, K. pneumoniae, P. aeruginosa (MICs = >8,000 mg/L for all), or L. monocytogenes (MIC = >3,000 mg/L). Elemicin is toxic to mice following metabolic activation to 1’-hydroxyelemicin by the cytochrome P450 (CYP) isoforms CYP1A1 and CYP1A2.{49623} It increases plasma and hepatic triglyceride levels, decreases stearoyl-CoA desaturase 1 (Scd1) expression, and induces hepatomegaly in mice when administered at a dose of 500 mg/kg per day for three weeks.
Brand:CaymanSKU:29394 - 1 gAvailable on backorder
Elemicin is a trioxygenated phenylpropane that has been found in A. dracunculus.{49622} It is active against S. aureus, B. subtilis, and C. albicans (MICs = 600, 2,500, and 1,000 mg/L, respectively) but not E. coli, K. pneumoniae, P. aeruginosa (MICs = >8,000 mg/L for all), or L. monocytogenes (MIC = >3,000 mg/L). Elemicin is toxic to mice following metabolic activation to 1’-hydroxyelemicin by the cytochrome P450 (CYP) isoforms CYP1A1 and CYP1A2.{49623} It increases plasma and hepatic triglyceride levels, decreases stearoyl-CoA desaturase 1 (Scd1) expression, and induces hepatomegaly in mice when administered at a dose of 500 mg/kg per day for three weeks.
Brand:CaymanSKU:29394 - 250 mgAvailable on backorder
Elemicin is a trioxygenated phenylpropane that has been found in A. dracunculus.{49622} It is active against S. aureus, B. subtilis, and C. albicans (MICs = 600, 2,500, and 1,000 mg/L, respectively) but not E. coli, K. pneumoniae, P. aeruginosa (MICs = >8,000 mg/L for all), or L. monocytogenes (MIC = >3,000 mg/L). Elemicin is toxic to mice following metabolic activation to 1’-hydroxyelemicin by the cytochrome P450 (CYP) isoforms CYP1A1 and CYP1A2.{49623} It increases plasma and hepatic triglyceride levels, decreases stearoyl-CoA desaturase 1 (Scd1) expression, and induces hepatomegaly in mice when administered at a dose of 500 mg/kg per day for three weeks.
Brand:CaymanSKU:29394 - 500 mgAvailable on backorder
Eletriptan is an agonist of the serotonin (5-HT) receptor types 5-HT1B and 5-HT1D.{32188} It inhibits forskolin-induced cAMP accumulation in and induces vasoconstriction of isolated rabbit common carotid artery rings (pD2s = 7.6 and 4.9, respectively), an effect that can be blocked by the 5-HT1B antagonist SB216641 but not the 5-HT1D antagonist BRL15572. Eletriptan preferentially induces constriction of isolated human cerebral over coronary arteries (EC50s = 15.8 and 1,995 nM, respectively).{42283} Formulations containing eletriptan have been used in the treatment of migraine headache.
Brand:CaymanSKU:20048 -Available on backorder
Eletriptan is an agonist of the serotonin (5-HT) receptor types 5-HT1B and 5-HT1D.{32188} It inhibits forskolin-induced cAMP accumulation in and induces vasoconstriction of isolated rabbit common carotid artery rings (pD2s = 7.6 and 4.9, respectively), an effect that can be blocked by the 5-HT1B antagonist SB216641 but not the 5-HT1D antagonist BRL15572. Eletriptan preferentially induces constriction of isolated human cerebral over coronary arteries (EC50s = 15.8 and 1,995 nM, respectively).{42283} Formulations containing eletriptan have been used in the treatment of migraine headache.
Brand:CaymanSKU:20048 -Available on backorder
Eletriptan is an agonist of the serotonin (5-HT) receptor types 5-HT1B and 5-HT1D.{32188} It inhibits forskolin-induced cAMP accumulation in and induces vasoconstriction of isolated rabbit common carotid artery rings (pD2s = 7.6 and 4.9, respectively), an effect that can be blocked by the 5-HT1B antagonist SB216641 but not the 5-HT1D antagonist BRL15572. Eletriptan preferentially induces constriction of isolated human cerebral over coronary arteries (EC50s = 15.8 and 1,995 nM, respectively).{42283} Formulations containing eletriptan have been used in the treatment of migraine headache.
Brand:CaymanSKU:20048 -Available on backorder
Eletriptan is an agonist of the serotonin (5-HT) receptor types 5-HT1B and 5-HT1D.{32188} It inhibits forskolin-induced cAMP accumulation in and induces vasoconstriction of isolated rabbit common carotid artery rings (pD2s = 7.6 and 4.9, respectively), an effect that can be blocked by the 5-HT1B antagonist SB216641 but not the 5-HT1D antagonist BRL15572. Eletriptan preferentially induces constriction of isolated human cerebral over coronary arteries (EC50s = 15.8 and 1,995 nM, respectively).{42283} Formulations containing eletriptan have been used in the treatment of migraine headache.
Brand:CaymanSKU:20048 -Available on backorder
Eleutheroside E is a glycoside and major component of E. senticosus and has diverse biological activities.{46673} It protects against axonal and dendritic atrophies induced by amyloid-β (25-35) (Aβ (25-35); Item No. 24155) in primary rat cortical neurons.{46673,46675,46674,46676} Eleutheroside E (15, 30, and 60 mg/kg) reduces macrophage infiltration, pannus formation, cartilage damage, bone erosion, and the production of TNF-α and IL-6 in a mouse model of collagen-induced arthritis.{46675} It increases insulin sensitivity and reduces pancreatic α- and β-cell death in db/db diabetic mice.{46674} Eleutheroside E (10 and 50 mg/kg) increases the latency to enter the dark chamber in a passive avoidance test and the levels of glutathione (GSH) in the hippocampus and decreases errors in the Y-maze test and hippocampal malondialdehyde (MDA) levels in a mouse model of sleep deprivation-induced stress.{46676}
Brand:CaymanSKU:29684 - 100 mgAvailable on backorder
Eleutheroside E is a glycoside and major component of E. senticosus and has diverse biological activities.{46673} It protects against axonal and dendritic atrophies induced by amyloid-β (25-35) (Aβ (25-35); Item No. 24155) in primary rat cortical neurons.{46673,46675,46674,46676} Eleutheroside E (15, 30, and 60 mg/kg) reduces macrophage infiltration, pannus formation, cartilage damage, bone erosion, and the production of TNF-α and IL-6 in a mouse model of collagen-induced arthritis.{46675} It increases insulin sensitivity and reduces pancreatic α- and β-cell death in db/db diabetic mice.{46674} Eleutheroside E (10 and 50 mg/kg) increases the latency to enter the dark chamber in a passive avoidance test and the levels of glutathione (GSH) in the hippocampus and decreases errors in the Y-maze test and hippocampal malondialdehyde (MDA) levels in a mouse model of sleep deprivation-induced stress.{46676}
Brand:CaymanSKU:29684 - 250 mgAvailable on backorder
Eleutheroside E is a glycoside and major component of E. senticosus and has diverse biological activities.{46673} It protects against axonal and dendritic atrophies induced by amyloid-β (25-35) (Aβ (25-35); Item No. 24155) in primary rat cortical neurons.{46673,46675,46674,46676} Eleutheroside E (15, 30, and 60 mg/kg) reduces macrophage infiltration, pannus formation, cartilage damage, bone erosion, and the production of TNF-α and IL-6 in a mouse model of collagen-induced arthritis.{46675} It increases insulin sensitivity and reduces pancreatic α- and β-cell death in db/db diabetic mice.{46674} Eleutheroside E (10 and 50 mg/kg) increases the latency to enter the dark chamber in a passive avoidance test and the levels of glutathione (GSH) in the hippocampus and decreases errors in the Y-maze test and hippocampal malondialdehyde (MDA) levels in a mouse model of sleep deprivation-induced stress.{46676}
Brand:CaymanSKU:29684 - 50 mgAvailable on backorder
Eleutheroside E is a glycoside and major component of E. senticosus and has diverse biological activities.{46673} It protects against axonal and dendritic atrophies induced by amyloid-β (25-35) (Aβ (25-35); Item No. 24155) in primary rat cortical neurons.{46673,46675,46674,46676} Eleutheroside E (15, 30, and 60 mg/kg) reduces macrophage infiltration, pannus formation, cartilage damage, bone erosion, and the production of TNF-α and IL-6 in a mouse model of collagen-induced arthritis.{46675} It increases insulin sensitivity and reduces pancreatic α- and β-cell death in db/db diabetic mice.{46674} Eleutheroside E (10 and 50 mg/kg) increases the latency to enter the dark chamber in a passive avoidance test and the levels of glutathione (GSH) in the hippocampus and decreases errors in the Y-maze test and hippocampal malondialdehyde (MDA) levels in a mouse model of sleep deprivation-induced stress.{46676}
Brand:CaymanSKU:29684 - 500 mgAvailable on backorder
Eliglustat is an inhibitor of glucosylceramide synthase (IC50 = 40 nM for inhibition of glucosylceramide production in K562 cells).{41053} It is selective for glucosylceramide synthase over α-glucosidase I and II, α-1,6-glucosidase, lysosomal glucocerebrosidase, non-lysosomal glucosylceramidase, sucrase, and maltase (IC50s = >10 µM for all). It decreases cell surface levels of the gangliosides GM1 and GM3 in K562 and B16/F10 cells with IC50 values of 24 and 29 nM, respectively. Eliglustat (150 mg/kg per day) decreases glucosylceramide levels in the liver and lungs of D409V/null mice, a model of Gaucher disease. Formulations containing eliglustat have been used in the treatment of type 1 Gaucher disease.
Brand:CaymanSKU:21487 -Out of stock
Eliglustat is an inhibitor of glucosylceramide synthase (IC50 = 40 nM for inhibition of glucosylceramide production in K562 cells).{41053} It is selective for glucosylceramide synthase over α-glucosidase I and II, α-1,6-glucosidase, lysosomal glucocerebrosidase, non-lysosomal glucosylceramidase, sucrase, and maltase (IC50s = >10 µM for all). It decreases cell surface levels of the gangliosides GM1 and GM3 in K562 and B16/F10 cells with IC50 values of 24 and 29 nM, respectively. Eliglustat (150 mg/kg per day) decreases glucosylceramide levels in the liver and lungs of D409V/null mice, a model of Gaucher disease. Formulations containing eliglustat have been used in the treatment of type 1 Gaucher disease.
Brand:CaymanSKU:21487 -Out of stock
Eliglustat is an inhibitor of glucosylceramide synthase (IC50 = 40 nM for inhibition of glucosylceramide production in K562 cells).{41053} It is selective for glucosylceramide synthase over α-glucosidase I and II, α-1,6-glucosidase, lysosomal glucocerebrosidase, non-lysosomal glucosylceramidase, sucrase, and maltase (IC50s = >10 µM for all). It decreases cell surface levels of the gangliosides GM1 and GM3 in K562 and B16/F10 cells with IC50 values of 24 and 29 nM, respectively. Eliglustat (150 mg/kg per day) decreases glucosylceramide levels in the liver and lungs of D409V/null mice, a model of Gaucher disease. Formulations containing eliglustat have been used in the treatment of type 1 Gaucher disease.
Brand:CaymanSKU:21487 -Out of stock
Eliglustat is an inhibitor of glucosylceramide synthase (IC50 = 40 nM for inhibition of glucosylceramide production in K562 cells).{41053} It is selective for glucosylceramide synthase over α-glucosidase I and II, α-1,6-glucosidase, lysosomal glucocerebrosidase, non-lysosomal glucosylceramidase, sucrase, and maltase (IC50s = >10 µM for all). It decreases cell surface levels of the gangliosides GM1 and GM3 in K562 and B16/F10 cells with IC50 values of 24 and 29 nM, respectively. Eliglustat (150 mg/kg per day) decreases glucosylceramide levels in the liver and lungs of D409V/null mice, a model of Gaucher disease. Formulations containing eliglustat have been used in the treatment of type 1 Gaucher disease.
Brand:CaymanSKU:21487 -Out of stock
Eliglustat-d15 is intended for use as an internal standard for the quantification of eliglustat (Item No. 21487) by GC- or LC-MS. Eliglustat is an inhibitor of glucosylceramide synthase (IC50 = 40 nM for inhibition of glucosylceramide production in K562 cells).{41053} It is selective for glucosylceramide synthase over α-glucosidase I and II, α-1,6-glucosidase, lysosomal glucocerebrosidase, non-lysosomal glucosylceramidase, sucrase, and maltase (IC50s = >10 µM for all). It decreases cell surface levels of the gangliosides GM1 and GM3 in K562 and B16/F10 cells with IC50 values of 24 and 29 nM, respectively. Eliglustat (150 mg/kg per day) decreases glucosylceramide levels in the liver and lungs of D409V/null mice, a model of Gaucher disease. Formulations containing eliglustat have been used in the treatment of type 1 Gaucher disease.
Brand:CaymanSKU:30167 - 1 mgAvailable on backorder
Eliglustat-d15 is intended for use as an internal standard for the quantification of eliglustat (Item No. 21487) by GC- or LC-MS. Eliglustat is an inhibitor of glucosylceramide synthase (IC50 = 40 nM for inhibition of glucosylceramide production in K562 cells).{41053} It is selective for glucosylceramide synthase over α-glucosidase I and II, α-1,6-glucosidase, lysosomal glucocerebrosidase, non-lysosomal glucosylceramidase, sucrase, and maltase (IC50s = >10 µM for all). It decreases cell surface levels of the gangliosides GM1 and GM3 in K562 and B16/F10 cells with IC50 values of 24 and 29 nM, respectively. Eliglustat (150 mg/kg per day) decreases glucosylceramide levels in the liver and lungs of D409V/null mice, a model of Gaucher disease. Formulations containing eliglustat have been used in the treatment of type 1 Gaucher disease.
Brand:CaymanSKU:30167 - 5 mgAvailable on backorder
Elinogrel is a reversible antagonist of the platelet purinergic P2Y12 receptor (Ki = 23 nM) that inhibits platelet aggregation in a human platelet-rich plasma (hPRP) assay (IC50 = 2.81 nM).{25099} It inhibits thrombosis in a mouse model of vascular injury induced by iron (III) chloride (FeCl3) when administered at a dose of 60 mg/kg.{45029}
Brand:CaymanSKU:25976 - 1 mgAvailable on backorder
Elinogrel is a reversible antagonist of the platelet purinergic P2Y12 receptor (Ki = 23 nM) that inhibits platelet aggregation in a human platelet-rich plasma (hPRP) assay (IC50 = 2.81 nM).{25099} It inhibits thrombosis in a mouse model of vascular injury induced by iron (III) chloride (FeCl3) when administered at a dose of 60 mg/kg.{45029}
Brand:CaymanSKU:25976 - 5 mgAvailable on backorder
N-Methyl-D-aspartate (NMDA) receptors are calcium permeable ligand-gated channels of the central nervous system that are activated after binding of the co-agonists glutamate and glycine. Eliprodil is a non-competitive NMDA receptor antagonist that inhibits neuronal calcium channel currents.{31071} It is selective for NR2B subunit-containing receptors (IC50 = 1 µM), displaying greater than 100-fold selectivity for NR2B over NR2A and NR2C subunits.{31074,31072} Eliprodil also avidly binds σ1 and σ2 sites (Kis = 0.013 and 0.63 µM, respectively).{31074} It is effective in vivo, blocking ischemia-induced neurodegeneration in the CA1 region of the hippocampus of gerbils subjected to bilateral carotid artery occlusion.{31071} Eliprodil can also have proarrhythmic actions in hearts under normal conditions.{31073}
Brand:CaymanSKU:-Available on backorder
N-Methyl-D-aspartate (NMDA) receptors are calcium permeable ligand-gated channels of the central nervous system that are activated after binding of the co-agonists glutamate and glycine. Eliprodil is a non-competitive NMDA receptor antagonist that inhibits neuronal calcium channel currents.{31071} It is selective for NR2B subunit-containing receptors (IC50 = 1 µM), displaying greater than 100-fold selectivity for NR2B over NR2A and NR2C subunits.{31074,31072} Eliprodil also avidly binds σ1 and σ2 sites (Kis = 0.013 and 0.63 µM, respectively).{31074} It is effective in vivo, blocking ischemia-induced neurodegeneration in the CA1 region of the hippocampus of gerbils subjected to bilateral carotid artery occlusion.{31071} Eliprodil can also have proarrhythmic actions in hearts under normal conditions.{31073}
Brand:CaymanSKU:-Available on backorder
N-Methyl-D-aspartate (NMDA) receptors are calcium permeable ligand-gated channels of the central nervous system that are activated after binding of the co-agonists glutamate and glycine. Eliprodil is a non-competitive NMDA receptor antagonist that inhibits neuronal calcium channel currents.{31071} It is selective for NR2B subunit-containing receptors (IC50 = 1 µM), displaying greater than 100-fold selectivity for NR2B over NR2A and NR2C subunits.{31074,31072} Eliprodil also avidly binds σ1 and σ2 sites (Kis = 0.013 and 0.63 µM, respectively).{31074} It is effective in vivo, blocking ischemia-induced neurodegeneration in the CA1 region of the hippocampus of gerbils subjected to bilateral carotid artery occlusion.{31071} Eliprodil can also have proarrhythmic actions in hearts under normal conditions.{31073}
Brand:CaymanSKU:-Available on backorder
N-Methyl-D-aspartate (NMDA) receptors are calcium permeable ligand-gated channels of the central nervous system that are activated after binding of the co-agonists glutamate and glycine. Eliprodil is a non-competitive NMDA receptor antagonist that inhibits neuronal calcium channel currents.{31071} It is selective for NR2B subunit-containing receptors (IC50 = 1 µM), displaying greater than 100-fold selectivity for NR2B over NR2A and NR2C subunits.{31074,31072} Eliprodil also avidly binds σ1 and σ2 sites (Kis = 0.013 and 0.63 µM, respectively).{31074} It is effective in vivo, blocking ischemia-induced neurodegeneration in the CA1 region of the hippocampus of gerbils subjected to bilateral carotid artery occlusion.{31071} Eliprodil can also have proarrhythmic actions in hearts under normal conditions.{31073}
Brand:CaymanSKU:-Available on backorder
This dye may be added to Cayman’s ELISA antisera if desired to aid in visualization of antiserum-containing wells.
Brand:CaymanSKU:400042 - 1 eaAvailable on backorder
Brand:CaymanSKU:400060 - 10 mlAvailable on backorder
Brand:CaymanSKU:400040 - 1 eaAvailable on backorder
Ellagic acid is a polyphenolic antioxidant that is abundant in many fruits, vegetables, plant bark, and peels. It has anti-carcinogenic, anti-mutagenic, anti-inflammatory, and organ-preserving properties, presumably related to its ability to alter cytochrome P450 activity and improve metabolism and clearance of xenobiotics, as well as alter immune function.{18587,18585,18586} Ellagic acid also blocks methylation of arginine 17 of histone 3 (H3R17) by coactivator-associated arginine methyltransferase 1 (CARM1) without significantly altering histone acetylase or DNA methyltransferase activity.{18399,18400,18401}
Brand:CaymanSKU:10569 - 1 gAvailable on backorder
Ellagic acid is a polyphenolic antioxidant that is abundant in many fruits, vegetables, plant bark, and peels. It has anti-carcinogenic, anti-mutagenic, anti-inflammatory, and organ-preserving properties, presumably related to its ability to alter cytochrome P450 activity and improve metabolism and clearance of xenobiotics, as well as alter immune function.{18587,18585,18586} Ellagic acid also blocks methylation of arginine 17 of histone 3 (H3R17) by coactivator-associated arginine methyltransferase 1 (CARM1) without significantly altering histone acetylase or DNA methyltransferase activity.{18399,18400,18401}
Brand:CaymanSKU:10569 - 100 mgAvailable on backorder
Ellagic acid is a polyphenolic antioxidant that is abundant in many fruits, vegetables, plant bark, and peels. It has anti-carcinogenic, anti-mutagenic, anti-inflammatory, and organ-preserving properties, presumably related to its ability to alter cytochrome P450 activity and improve metabolism and clearance of xenobiotics, as well as alter immune function.{18587,18585,18586} Ellagic acid also blocks methylation of arginine 17 of histone 3 (H3R17) by coactivator-associated arginine methyltransferase 1 (CARM1) without significantly altering histone acetylase or DNA methyltransferase activity.{18399,18400,18401}
Brand:CaymanSKU:10569 - 500 mgAvailable on backorder
Ellipticine is an alkaloid isolated from Apocyanaceae plants that exhibits antitumor activities by intercalating into DNA and/or inhibiting DNA topoisomerase II.{30281,30282,30280} It forms covalent adducts in DNA after being enzymatically activated with cytochrome P450 isoforms (e.g., CYP3A4, CYP1A1, or CYP1A2) or by peroxidases in target tissues.{30282,30280} Ellipticine has been shown to inhibit the proliferation of human breast adenocarcinoma MCF-7 cells, leukemia HL-60 and CCRF-CEM cells, neuroblastoma IMR-32, UKF-NB-3, and UKF-NB-4 cells, and U87MG glioblastoma cells with IC50 values ranging from 0.27-4.7 µM.{30282}
Brand:CaymanSKU:-Available on backorder
Ellipticine is an alkaloid isolated from Apocyanaceae plants that exhibits antitumor activities by intercalating into DNA and/or inhibiting DNA topoisomerase II.{30281,30282,30280} It forms covalent adducts in DNA after being enzymatically activated with cytochrome P450 isoforms (e.g., CYP3A4, CYP1A1, or CYP1A2) or by peroxidases in target tissues.{30282,30280} Ellipticine has been shown to inhibit the proliferation of human breast adenocarcinoma MCF-7 cells, leukemia HL-60 and CCRF-CEM cells, neuroblastoma IMR-32, UKF-NB-3, and UKF-NB-4 cells, and U87MG glioblastoma cells with IC50 values ranging from 0.27-4.7 µM.{30282}
Brand:CaymanSKU:-Available on backorder
Ellipticine is an alkaloid isolated from Apocyanaceae plants that exhibits antitumor activities by intercalating into DNA and/or inhibiting DNA topoisomerase II.{30281,30282,30280} It forms covalent adducts in DNA after being enzymatically activated with cytochrome P450 isoforms (e.g., CYP3A4, CYP1A1, or CYP1A2) or by peroxidases in target tissues.{30282,30280} Ellipticine has been shown to inhibit the proliferation of human breast adenocarcinoma MCF-7 cells, leukemia HL-60 and CCRF-CEM cells, neuroblastoma IMR-32, UKF-NB-3, and UKF-NB-4 cells, and U87MG glioblastoma cells with IC50 values ranging from 0.27-4.7 µM.{30282}
Brand:CaymanSKU:-Available on backorder
Ellipticine is an alkaloid isolated from Apocyanaceae plants that exhibits antitumor activities by intercalating into DNA and/or inhibiting DNA topoisomerase II.{30281,30282,30280} It forms covalent adducts in DNA after being enzymatically activated with cytochrome P450 isoforms (e.g., CYP3A4, CYP1A1, or CYP1A2) or by peroxidases in target tissues.{30282,30280} Ellipticine has been shown to inhibit the proliferation of human breast adenocarcinoma MCF-7 cells, leukemia HL-60 and CCRF-CEM cells, neuroblastoma IMR-32, UKF-NB-3, and UKF-NB-4 cells, and U87MG glioblastoma cells with IC50 values ranging from 0.27-4.7 µM.{30282}
Brand:CaymanSKU:-Available on backorder
ELR510444 is an inhibitor of tubulin polymerization (IC50 = 10 μM) that binds to tubulin at the colchicine (Item No. 9000760) binding site.{38488} It induces microtubule depolymerization in A-10 cells (EC50 = 21 nM). ELR510444 inhibits growth in a cancer cell line panel (IC50s = 9-43 nM) via formation of multiple spindles and induction of mitotic arrest. Oral administration of ELR510444 (3-6 mg/kg) reduces tumor size in an MDA-MB-231 breast cancer mouse xenograft model in a dose-dependent manner. ELR510444 also inhibits hypoxia-inducible factor 1α (HIF-1α) in RCC4 cells in a concentration-dependent manner.{38487}
Brand:CaymanSKU:-Available on backorder
ELR510444 is an inhibitor of tubulin polymerization (IC50 = 10 μM) that binds to tubulin at the colchicine (Item No. 9000760) binding site.{38488} It induces microtubule depolymerization in A-10 cells (EC50 = 21 nM). ELR510444 inhibits growth in a cancer cell line panel (IC50s = 9-43 nM) via formation of multiple spindles and induction of mitotic arrest. Oral administration of ELR510444 (3-6 mg/kg) reduces tumor size in an MDA-MB-231 breast cancer mouse xenograft model in a dose-dependent manner. ELR510444 also inhibits hypoxia-inducible factor 1α (HIF-1α) in RCC4 cells in a concentration-dependent manner.{38487}
Brand:CaymanSKU:-Available on backorder
ELR510444 is an inhibitor of tubulin polymerization (IC50 = 10 μM) that binds to tubulin at the colchicine (Item No. 9000760) binding site.{38488} It induces microtubule depolymerization in A-10 cells (EC50 = 21 nM). ELR510444 inhibits growth in a cancer cell line panel (IC50s = 9-43 nM) via formation of multiple spindles and induction of mitotic arrest. Oral administration of ELR510444 (3-6 mg/kg) reduces tumor size in an MDA-MB-231 breast cancer mouse xenograft model in a dose-dependent manner. ELR510444 also inhibits hypoxia-inducible factor 1α (HIF-1α) in RCC4 cells in a concentration-dependent manner.{38487}
Brand:CaymanSKU:-Available on backorder
ELR510444 is an inhibitor of tubulin polymerization (IC50 = 10 μM) that binds to tubulin at the colchicine (Item No. 9000760) binding site.{38488} It induces microtubule depolymerization in A-10 cells (EC50 = 21 nM). ELR510444 inhibits growth in a cancer cell line panel (IC50s = 9-43 nM) via formation of multiple spindles and induction of mitotic arrest. Oral administration of ELR510444 (3-6 mg/kg) reduces tumor size in an MDA-MB-231 breast cancer mouse xenograft model in a dose-dependent manner. ELR510444 also inhibits hypoxia-inducible factor 1α (HIF-1α) in RCC4 cells in a concentration-dependent manner.{38487}
Brand:CaymanSKU:-Available on backorder
Eltenac is a non-selective COX inhibitor (IC50 = 0.03 µM for both COX-1 and COX-2 in isolated human whole blood) and a non-steroidal anti-inflammatory drug (NSAID).{55033} In vivo, eltenac (1 mg/kg) reduces lameness in horses with tendinitis, pododermatitis, navicular disease, non-infectious arthritis, degenerative joint disease, phalanx fracture, and osteochondrosis.{55034} It also reduces castration-induced edema in horses. Formulations containing eltenac have been used in the treatment of postoperative swelling in horses.
Brand:CaymanSKU:27673 - 1 mgAvailable on backorder
Eltenac is a non-selective COX inhibitor (IC50 = 0.03 µM for both COX-1 and COX-2 in isolated human whole blood) and a non-steroidal anti-inflammatory drug (NSAID).{55033} In vivo, eltenac (1 mg/kg) reduces lameness in horses with tendinitis, pododermatitis, navicular disease, non-infectious arthritis, degenerative joint disease, phalanx fracture, and osteochondrosis.{55034} It also reduces castration-induced edema in horses. Formulations containing eltenac have been used in the treatment of postoperative swelling in horses.
Brand:CaymanSKU:27673 - 5 mgAvailable on backorder
Eltenac is a non-selective COX inhibitor (IC50 = 0.03 µM for both COX-1 and COX-2 in isolated human whole blood) and a non-steroidal anti-inflammatory drug (NSAID).{55033} In vivo, eltenac (1 mg/kg) reduces lameness in horses with tendinitis, pododermatitis, navicular disease, non-infectious arthritis, degenerative joint disease, phalanx fracture, and osteochondrosis.{55034} It also reduces castration-induced edema in horses. Formulations containing eltenac have been used in the treatment of postoperative swelling in horses.
Brand:CaymanSKU:27673 - 500 µgAvailable on backorder
Eltoprazine is a phenylpiperazine compound that acts as a partial agonist at serotonin 5-HT1A, 5-HT1B, and 5-HT2B receptors (Kis = 40, 52, and 81 nM, respectively).{29966} It exerts a dose-dependent decrease in aggressive behavior in resident-intruder tests with rats (ID50 = 0.24 mg/kg).{29965}
Brand:CaymanSKU:-Available on backorder
Eltoprazine is a phenylpiperazine compound that acts as a partial agonist at serotonin 5-HT1A, 5-HT1B, and 5-HT2B receptors (Kis = 40, 52, and 81 nM, respectively).{29966} It exerts a dose-dependent decrease in aggressive behavior in resident-intruder tests with rats (ID50 = 0.24 mg/kg).{29965}
Brand:CaymanSKU:-Available on backorder
Eltoprazine is a phenylpiperazine compound that acts as a partial agonist at serotonin 5-HT1A, 5-HT1B, and 5-HT2B receptors (Kis = 40, 52, and 81 nM, respectively).{29966} It exerts a dose-dependent decrease in aggressive behavior in resident-intruder tests with rats (ID50 = 0.24 mg/kg).{29965}
Brand:CaymanSKU:-Available on backorder
Eltoprazine is a phenylpiperazine compound that acts as a partial agonist at serotonin 5-HT1A, 5-HT1B, and 5-HT2B receptors (Kis = 40, 52, and 81 nM, respectively).{29966} It exerts a dose-dependent decrease in aggressive behavior in resident-intruder tests with rats (ID50 = 0.24 mg/kg).{29965}
Brand:CaymanSKU:-Available on backorder
Eltrombopag is an orally bioavailable nonpeptide agonist of the thrombopoietin receptor (EC50 = 0.27 µM in a reporter assay) and an iron chelator.{16951} It increases STAT5 phosphorylation in N2C-Tpo cells when used at a concentration of 30 µM and p42/44 MAPK phosphorylation when used at 10 µM. Eltrombopag binds to the transmembrane domain of the thrombopoietin receptor and stimulates megakaryocytopoiesis in human primary bone marrow cells. It increases platelet production in chimpanzees when administered at a dose of 10 mg/kg per day for five days. Eltrombopag also binds to iron (III) and mobilizes cellular iron and ferritin in H9C2, Huh7, and RINm5F cells in a concentration-dependent manner.{47035} It enhances cellular iron mobilization when used in combination with the iron chelators deferasirox (Item No. 16753) and CP40.
Brand:CaymanSKU:- Eltrombopag is an orally bioavailable nonpeptide agonist of the thrombopoietin receptor (EC50 = 0.27 µM in a reporter assay) and an iron chelator.{16951} It increases STAT5 phosphorylation in N2C-Tpo cells when used at a concentration of 30 µM and p42/44 MAPK phosphorylation when used at 10 µM. Eltrombopag binds to the transmembrane domain of the thrombopoietin receptor and stimulates megakaryocytopoiesis in human primary bone marrow cells. It increases platelet production in chimpanzees when administered at a dose of 10 mg/kg per day for five days. Eltrombopag also binds to iron (III) and mobilizes cellular iron and ferritin in H9C2, Huh7, and RINm5F cells in a concentration-dependent manner.{47035} It enhances cellular iron mobilization when used in combination with the iron chelators deferasirox (Item No. 16753) and CP40.
Brand:CaymanSKU:- Eltrombopag is an orally bioavailable nonpeptide agonist of the thrombopoietin receptor (EC50 = 0.27 µM in a reporter assay) and an iron chelator.{16951} It increases STAT5 phosphorylation in N2C-Tpo cells when used at a concentration of 30 µM and p42/44 MAPK phosphorylation when used at 10 µM. Eltrombopag binds to the transmembrane domain of the thrombopoietin receptor and stimulates megakaryocytopoiesis in human primary bone marrow cells. It increases platelet production in chimpanzees when administered at a dose of 10 mg/kg per day for five days. Eltrombopag also binds to iron (III) and mobilizes cellular iron and ferritin in H9C2, Huh7, and RINm5F cells in a concentration-dependent manner.{47035} It enhances cellular iron mobilization when used in combination with the iron chelators deferasirox (Item No. 16753) and CP40.
Brand:CaymanSKU:- Eltrombopag is an orally bioavailable nonpeptide agonist of the thrombopoietin receptor (EC50 = 0.27 µM in a reporter assay) and an iron chelator.{16951} It increases STAT5 phosphorylation in N2C-Tpo cells when used at a concentration of 30 µM and p42/44 MAPK phosphorylation when used at 10 µM. Eltrombopag binds to the transmembrane domain of the thrombopoietin receptor and stimulates megakaryocytopoiesis in human primary bone marrow cells. It increases platelet production in chimpanzees when administered at a dose of 10 mg/kg per day for five days. Eltrombopag also binds to iron (III) and mobilizes cellular iron and ferritin in H9C2, Huh7, and RINm5F cells in a concentration-dependent manner.{47035} It enhances cellular iron mobilization when used in combination with the iron chelators deferasirox (Item No. 16753) and CP40.
Brand:CaymanSKU:-
Elvitegravir is a quinolone antibiotic that inhibits HIV-1 integrase (IC50 = 7.2 nM).{29011} It has antiviral activity against laboratory strains and clinical isolates of HIV-1 in MAGI cells (EC50s = 0.1-1.26 nM) and HIV-2 in peripheral blood mononuclear cells (PBMCs; EC50s = 0.3-0.9).{20011,42943} Formulations containing elvitegravir have been used in the treatment of HIV infections.
Brand:CaymanSKU:-Available on backorder
Elvitegravir is a quinolone antibiotic that inhibits HIV-1 integrase (IC50 = 7.2 nM).{29011} It has antiviral activity against laboratory strains and clinical isolates of HIV-1 in MAGI cells (EC50s = 0.1-1.26 nM) and HIV-2 in peripheral blood mononuclear cells (PBMCs; EC50s = 0.3-0.9).{20011,42943} Formulations containing elvitegravir have been used in the treatment of HIV infections.
Brand:CaymanSKU:-Available on backorder
Elvitegravir is a quinolone antibiotic that inhibits HIV-1 integrase (IC50 = 7.2 nM).{29011} It has antiviral activity against laboratory strains and clinical isolates of HIV-1 in MAGI cells (EC50s = 0.1-1.26 nM) and HIV-2 in peripheral blood mononuclear cells (PBMCs; EC50s = 0.3-0.9).{20011,42943} Formulations containing elvitegravir have been used in the treatment of HIV infections.
Brand:CaymanSKU:-Available on backorder
Elvitegravir is a quinolone antibiotic that inhibits HIV-1 integrase (IC50 = 7.2 nM).{29011} It has antiviral activity against laboratory strains and clinical isolates of HIV-1 in MAGI cells (EC50s = 0.1-1.26 nM) and HIV-2 in peripheral blood mononuclear cells (PBMCs; EC50s = 0.3-0.9).{20011,42943} Formulations containing elvitegravir have been used in the treatment of HIV infections.
Brand:CaymanSKU:-Available on backorder
EM574 is a motilin receptor agonist with an IC50 value of 6.17 nM for binding to rabbit gastric antral smooth muscle homogenates in a radioligand binding assay.{45198} It also binds to human smooth muscle homogenates in a radioligand binding assay (Kd = 7.8 nM).{45199} EM574 induces contraction of isolated rabbit, but not rat or guinea pig, intestine (EC50 = 5.5 nM).{45198} It increases antral motility and enhances gastric emptying in canine models of gastroparesis when administered intraduodenally at a dose of 0.03 mg/kg following a semi-solid meal.{45200}
Brand:CaymanSKU:27752 - 1 mgAvailable on backorder
EM574 is a motilin receptor agonist with an IC50 value of 6.17 nM for binding to rabbit gastric antral smooth muscle homogenates in a radioligand binding assay.{45198} It also binds to human smooth muscle homogenates in a radioligand binding assay (Kd = 7.8 nM).{45199} EM574 induces contraction of isolated rabbit, but not rat or guinea pig, intestine (EC50 = 5.5 nM).{45198} It increases antral motility and enhances gastric emptying in canine models of gastroparesis when administered intraduodenally at a dose of 0.03 mg/kg following a semi-solid meal.{45200}
Brand:CaymanSKU:27752 - 500 µgAvailable on backorder
EMA401 is an orally bioavailable and selective antagonist of the angiotensin II type 2 receptor (AT2; IC50s = 39.5 and 408,000 nM for rat recombinant AT2 and AT1, respectively).{47001} It inhibits capsaicin-induced calcium influx in cultured human dorsal root ganglion (hDRG) neurons (IC50 = 10 nM) and reduces neurite density and length in rat DRG neuronal cultures.{47002} EMA401 has analgesic effects in a rat model of neuropathic pain induced by chronic constriction injury.{47003}
Brand:CaymanSKU:22988 - 1 mgAvailable on backorder
EMA401 is an orally bioavailable and selective antagonist of the angiotensin II type 2 receptor (AT2; IC50s = 39.5 and 408,000 nM for rat recombinant AT2 and AT1, respectively).{47001} It inhibits capsaicin-induced calcium influx in cultured human dorsal root ganglion (hDRG) neurons (IC50 = 10 nM) and reduces neurite density and length in rat DRG neuronal cultures.{47002} EMA401 has analgesic effects in a rat model of neuropathic pain induced by chronic constriction injury.{47003}
Brand:CaymanSKU:22988 - 10 mgAvailable on backorder
EMA401 is an orally bioavailable and selective antagonist of the angiotensin II type 2 receptor (AT2; IC50s = 39.5 and 408,000 nM for rat recombinant AT2 and AT1, respectively).{47001} It inhibits capsaicin-induced calcium influx in cultured human dorsal root ganglion (hDRG) neurons (IC50 = 10 nM) and reduces neurite density and length in rat DRG neuronal cultures.{47002} EMA401 has analgesic effects in a rat model of neuropathic pain induced by chronic constriction injury.{47003}
Brand:CaymanSKU:22988 - 25 mgAvailable on backorder
EMA401 is an orally bioavailable and selective antagonist of the angiotensin II type 2 receptor (AT2; IC50s = 39.5 and 408,000 nM for rat recombinant AT2 and AT1, respectively).{47001} It inhibits capsaicin-induced calcium influx in cultured human dorsal root ganglion (hDRG) neurons (IC50 = 10 nM) and reduces neurite density and length in rat DRG neuronal cultures.{47002} EMA401 has analgesic effects in a rat model of neuropathic pain induced by chronic constriction injury.{47003}
Brand:CaymanSKU:22988 - 5 mgAvailable on backorder
Emamectin B1a is a semi-synthetic derivative of avermectin B1a (Item No. 22000).{35148} It binds to GABAA receptors (Ki = 17.6 nM in rat brain membranes), including those containing β1, β2, or β3 subunits (IC50s = 57, 210, and 49.8 nM for α1β1γ2, α1β2γ2, and α1β3γ2 subunits, respectively), and potentiates the GABA response.{35146} Emamectin B1a also binds to and inhibits glycine receptors (IC50 = 218 nM in rat spinal cord). Emamectin B1a induces mortality in 90% of S. exigua larvae in a diet incorporation assay at a dose of 1.067 ng/ml, which is approximately 1,500-fold more toxic than avermectin B1. It is effective against neonate S. eridania larvae in a foliage spray bioassay and when applied topically.
Brand:CaymanSKU:24060 - 1 mgAvailable on backorder
Emamectin B1a is a semi-synthetic derivative of avermectin B1a (Item No. 22000).{35148} It binds to GABAA receptors (Ki = 17.6 nM in rat brain membranes), including those containing β1, β2, or β3 subunits (IC50s = 57, 210, and 49.8 nM for α1β1γ2, α1β2γ2, and α1β3γ2 subunits, respectively), and potentiates the GABA response.{35146} Emamectin B1a also binds to and inhibits glycine receptors (IC50 = 218 nM in rat spinal cord). Emamectin B1a induces mortality in 90% of S. exigua larvae in a diet incorporation assay at a dose of 1.067 ng/ml, which is approximately 1,500-fold more toxic than avermectin B1. It is effective against neonate S. eridania larvae in a foliage spray bioassay and when applied topically.
Brand:CaymanSKU:24060 - 5 mgAvailable on backorder
X-Linked inhibitor of apoptosis (XIAP) is a protein which modulates several pathways, including several related to apoptosis.{21506} Embelin is a natural benzoquinone, isolated from plants of the genus Embelia, which directly binds and inhibits XIAP (IC50 = 4.1 μM).{21510} In this way, this cell-permeable inhibitor blocks growth while activating caspases and promoting apoptosis in cancer cells expressing high levels of XIAP.{21510} Presumably in an XIAP-dependent fashion, embelin (15-50 μM) also prevents NF-κB activation by inhibiting IKK.{21505,21511} This compound also protects against XIAP- and caspase-dependent inflammation.{21509,21512}
Brand:CaymanSKU:11838 - 10 mgAvailable on backorder
X-Linked inhibitor of apoptosis (XIAP) is a protein which modulates several pathways, including several related to apoptosis.{21506} Embelin is a natural benzoquinone, isolated from plants of the genus Embelia, which directly binds and inhibits XIAP (IC50 = 4.1 μM).{21510} In this way, this cell-permeable inhibitor blocks growth while activating caspases and promoting apoptosis in cancer cells expressing high levels of XIAP.{21510} Presumably in an XIAP-dependent fashion, embelin (15-50 μM) also prevents NF-κB activation by inhibiting IKK.{21505,21511} This compound also protects against XIAP- and caspase-dependent inflammation.{21509,21512}
Brand:CaymanSKU:11838 - 100 mgAvailable on backorder
X-Linked inhibitor of apoptosis (XIAP) is a protein which modulates several pathways, including several related to apoptosis.{21506} Embelin is a natural benzoquinone, isolated from plants of the genus Embelia, which directly binds and inhibits XIAP (IC50 = 4.1 μM).{21510} In this way, this cell-permeable inhibitor blocks growth while activating caspases and promoting apoptosis in cancer cells expressing high levels of XIAP.{21510} Presumably in an XIAP-dependent fashion, embelin (15-50 μM) also prevents NF-κB activation by inhibiting IKK.{21505,21511} This compound also protects against XIAP- and caspase-dependent inflammation.{21509,21512}
Brand:CaymanSKU:11838 - 50 mgAvailable 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. EMD 1214063 inhibits c-Met with an IC50 value of 3 nM, demonstrating at least 1,000-fold selectivity for c-Met over a panel of 242 additional kinases.{29889} It has been shown to inhibit c-Met phosphorylation and downstream signaling in various cancer cell lines (IC50s = 6-9 nM) and, at 5-15 mg/kg, to regress tumors in mouse xenograft models.{29889}
Brand:CaymanSKU:-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. EMD 1214063 inhibits c-Met with an IC50 value of 3 nM, demonstrating at least 1,000-fold selectivity for c-Met over a panel of 242 additional kinases.{29889} It has been shown to inhibit c-Met phosphorylation and downstream signaling in various cancer cell lines (IC50s = 6-9 nM) and, at 5-15 mg/kg, to regress tumors in mouse xenograft models.{29889}
Brand:CaymanSKU:-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. EMD 1214063 inhibits c-Met with an IC50 value of 3 nM, demonstrating at least 1,000-fold selectivity for c-Met over a panel of 242 additional kinases.{29889} It has been shown to inhibit c-Met phosphorylation and downstream signaling in various cancer cell lines (IC50s = 6-9 nM) and, at 5-15 mg/kg, to regress tumors in mouse xenograft models.{29889}
Brand:CaymanSKU:-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. EMD 1214063 inhibits c-Met with an IC50 value of 3 nM, demonstrating at least 1,000-fold selectivity for c-Met over a panel of 242 additional kinases.{29889} It has been shown to inhibit c-Met phosphorylation and downstream signaling in various cancer cell lines (IC50s = 6-9 nM) and, at 5-15 mg/kg, to regress tumors in mouse xenograft models.{29889}
Brand:CaymanSKU:-Available on backorder
EMD 638683 is an inhibitor of serum- and glucocorticoid-regulated kinase 1 (SGK1) that inhibits SGK1 by 85% when used at a concentration of 1 µM.{59340} It is greater than 27-fold selective for SGK1 over a panel of 11 kinases but does inhibit SGK2, SGK3, PRK2, and MSK1 by greater than 50% at 1 µM. EMD 638683 inhibits phosphorylation of the SGK1 target NDRG1 in HeLa cells (IC50 = 3.35 µM). It increases radiation-induced apoptosis of Caco-2 colon carcinoma cells when used at a concentration of 50 µM.{59341} Dietary administration of EMD 638683 (600 mg/kg) reduces the number of tumors in a mouse model of chemical carcinogenesis. It prevents fructose and saline consumption-induced increases in systolic blood pressure in mice.{59340} EMD 638683 decreases body weight, fasting blood glucose and hemoglobin A1c (HbA1C) levels, and food intake in db/db diabetic mice.{59342} It also reduces angiotensin II-induced collagen deposition and cardiac fibrosis in mice.{59343}
Brand:CaymanSKU:31117 - 1 mgAvailable on backorder
EMD 638683 is an inhibitor of serum- and glucocorticoid-regulated kinase 1 (SGK1) that inhibits SGK1 by 85% when used at a concentration of 1 µM.{59340} It is greater than 27-fold selective for SGK1 over a panel of 11 kinases but does inhibit SGK2, SGK3, PRK2, and MSK1 by greater than 50% at 1 µM. EMD 638683 inhibits phosphorylation of the SGK1 target NDRG1 in HeLa cells (IC50 = 3.35 µM). It increases radiation-induced apoptosis of Caco-2 colon carcinoma cells when used at a concentration of 50 µM.{59341} Dietary administration of EMD 638683 (600 mg/kg) reduces the number of tumors in a mouse model of chemical carcinogenesis. It prevents fructose and saline consumption-induced increases in systolic blood pressure in mice.{59340} EMD 638683 decreases body weight, fasting blood glucose and hemoglobin A1c (HbA1C) levels, and food intake in db/db diabetic mice.{59342} It also reduces angiotensin II-induced collagen deposition and cardiac fibrosis in mice.{59343}
Brand:CaymanSKU:31117 - 10 mgAvailable on backorder
EMD 638683 is an inhibitor of serum- and glucocorticoid-regulated kinase 1 (SGK1) that inhibits SGK1 by 85% when used at a concentration of 1 µM.{59340} It is greater than 27-fold selective for SGK1 over a panel of 11 kinases but does inhibit SGK2, SGK3, PRK2, and MSK1 by greater than 50% at 1 µM. EMD 638683 inhibits phosphorylation of the SGK1 target NDRG1 in HeLa cells (IC50 = 3.35 µM). It increases radiation-induced apoptosis of Caco-2 colon carcinoma cells when used at a concentration of 50 µM.{59341} Dietary administration of EMD 638683 (600 mg/kg) reduces the number of tumors in a mouse model of chemical carcinogenesis. It prevents fructose and saline consumption-induced increases in systolic blood pressure in mice.{59340} EMD 638683 decreases body weight, fasting blood glucose and hemoglobin A1c (HbA1C) levels, and food intake in db/db diabetic mice.{59342} It also reduces angiotensin II-induced collagen deposition and cardiac fibrosis in mice.{59343}
Brand:CaymanSKU:31117 - 25 mgAvailable on backorder
EMD 638683 is an inhibitor of serum- and glucocorticoid-regulated kinase 1 (SGK1) that inhibits SGK1 by 85% when used at a concentration of 1 µM.{59340} It is greater than 27-fold selective for SGK1 over a panel of 11 kinases but does inhibit SGK2, SGK3, PRK2, and MSK1 by greater than 50% at 1 µM. EMD 638683 inhibits phosphorylation of the SGK1 target NDRG1 in HeLa cells (IC50 = 3.35 µM). It increases radiation-induced apoptosis of Caco-2 colon carcinoma cells when used at a concentration of 50 µM.{59341} Dietary administration of EMD 638683 (600 mg/kg) reduces the number of tumors in a mouse model of chemical carcinogenesis. It prevents fructose and saline consumption-induced increases in systolic blood pressure in mice.{59340} EMD 638683 decreases body weight, fasting blood glucose and hemoglobin A1c (HbA1C) levels, and food intake in db/db diabetic mice.{59342} It also reduces angiotensin II-induced collagen deposition and cardiac fibrosis in mice.{59343}
Brand:CaymanSKU:31117 - 5 mgAvailable on backorder
Emedastine is a potent and selective histamine H1 receptor antagonist with 37,744-fold and 9,562-fold selectivity over H2 and H3, respectively (Kis = 1.3, 49,067, and 12,430 nM for H1, H2, and H3, respectively).{38529} It is selective for H1 receptors with less than 50% inhibition of α1-, α2-, and β1-adrenergic, dopamine D1 and D2, and serotonin 5-HT1 and 5-HT2 receptors at a concentration of 10 µM.{38530} It inhibits histamine-induced phosphoinositide turnover and intracellular calcium mobilization in primary human conjunctival epithelial cells (HCECs; IC50s = 1.6 and 2.9 nM, respectively).{38531} Emedastine inhibits histamine-stimulated cytokine secretion by primary HCECs, including IL-6, IL-8, and GM-CSF secretion (IC50s = 2.23, 3.42, and 1.50 nM, respectively).{38532} In guinea pigs, ocular application of emedastine 4 hours after histamine challenge inhibits vascular permeability with an ED50 value of 0.019% w/v.{38530} Formulations containing emedastine have been used in the treatment of allergic conjunctivitis.
Brand:CaymanSKU:23946 - 10 mgAvailable on backorder
Emedastine is a potent and selective histamine H1 receptor antagonist with 37,744-fold and 9,562-fold selectivity over H2 and H3, respectively (Kis = 1.3, 49,067, and 12,430 nM for H1, H2, and H3, respectively).{38529} It is selective for H1 receptors with less than 50% inhibition of α1-, α2-, and β1-adrenergic, dopamine D1 and D2, and serotonin 5-HT1 and 5-HT2 receptors at a concentration of 10 µM.{38530} It inhibits histamine-induced phosphoinositide turnover and intracellular calcium mobilization in primary human conjunctival epithelial cells (HCECs; IC50s = 1.6 and 2.9 nM, respectively).{38531} Emedastine inhibits histamine-stimulated cytokine secretion by primary HCECs, including IL-6, IL-8, and GM-CSF secretion (IC50s = 2.23, 3.42, and 1.50 nM, respectively).{38532} In guinea pigs, ocular application of emedastine 4 hours after histamine challenge inhibits vascular permeability with an ED50 value of 0.019% w/v.{38530} Formulations containing emedastine have been used in the treatment of allergic conjunctivitis.
Brand:CaymanSKU:23946 - 25 mgAvailable on backorder
Emedastine is a potent and selective histamine H1 receptor antagonist with 37,744-fold and 9,562-fold selectivity over H2 and H3, respectively (Kis = 1.3, 49,067, and 12,430 nM for H1, H2, and H3, respectively).{38529} It is selective for H1 receptors with less than 50% inhibition of α1-, α2-, and β1-adrenergic, dopamine D1 and D2, and serotonin 5-HT1 and 5-HT2 receptors at a concentration of 10 µM.{38530} It inhibits histamine-induced phosphoinositide turnover and intracellular calcium mobilization in primary human conjunctival epithelial cells (HCECs; IC50s = 1.6 and 2.9 nM, respectively).{38531} Emedastine inhibits histamine-stimulated cytokine secretion by primary HCECs, including IL-6, IL-8, and GM-CSF secretion (IC50s = 2.23, 3.42, and 1.50 nM, respectively).{38532} In guinea pigs, ocular application of emedastine 4 hours after histamine challenge inhibits vascular permeability with an ED50 value of 0.019% w/v.{38530} Formulations containing emedastine have been used in the treatment of allergic conjunctivitis.
Brand:CaymanSKU:23946 - 5 mgAvailable on backorder
Emedastine is a potent and selective histamine H1 receptor antagonist with 37,744-fold and 9,562-fold selectivity over H2 and H3, respectively (Kis = 1.3, 49,067, and 12,430 nM for H1, H2, and H3, respectively).{38529} It is selective for H1 receptors with less than 50% inhibition of α1-, α2-, and β1-adrenergic, dopamine D1 and D2, and serotonin 5-HT1 and 5-HT2 receptors at a concentration of 10 µM.{38530} It inhibits histamine-induced phosphoinositide turnover and intracellular calcium mobilization in primary human conjunctival epithelial cells (HCECs; IC50s = 1.6 and 2.9 nM, respectively).{38531} Emedastine inhibits histamine-stimulated cytokine secretion by primary HCECs, including IL-6, IL-8, and GM-CSF secretion (IC50s = 2.23, 3.42, and 1.50 nM, respectively).{38532} In guinea pigs, ocular application of emedastine 4 hours after histamine challenge inhibits vascular permeability with an ED50 value of 0.019% w/v.{38530} Formulations containing emedastine have been used in the treatment of allergic conjunctivitis.
Brand:CaymanSKU:23946 - 50 mgAvailable on backorder
Emestrin is a mycotoxin originally isolated from E. striata that has antimicrobial, immunomodulatory, and cytotoxic activities.{48878,48879,48880,48881,48882} It is active against the fungi C. albicans and C. neoformans, as well as the bacteria E. coli, S. aureus, and methicillin-resistant S. aureus (MRSA; IC50s = 3.94, 0.6, 2.21, 4.55, and 2.21 µg/ml, respectively).{48879} Emestrin is a chemokine (C-C motif) receptor 2 (CCR2) antagonist (IC50 = 5.4 µM in a radioligand binding assay using isolated human monocytes).{48880} Emestrin (0.1 µg/ml) induces apoptosis in HL-60 cells.{48881} It induces heart, thymus, and liver tissue necrosis in mice when administered at doses ranging from 18 to 30 mg/kg.{48882}
Brand:CaymanSKU:29970 - 1 mgAvailable on backorder
Emestrin is a mycotoxin originally isolated from E. striata that has antimicrobial, immunomodulatory, and cytotoxic activities.{48878,48879,48880,48881,48882} It is active against the fungi C. albicans and C. neoformans, as well as the bacteria E. coli, S. aureus, and methicillin-resistant S. aureus (MRSA; IC50s = 3.94, 0.6, 2.21, 4.55, and 2.21 µg/ml, respectively).{48879} Emestrin is a chemokine (C-C motif) receptor 2 (CCR2) antagonist (IC50 = 5.4 µM in a radioligand binding assay using isolated human monocytes).{48880} Emestrin (0.1 µg/ml) induces apoptosis in HL-60 cells.{48881} It induces heart, thymus, and liver tissue necrosis in mice when administered at doses ranging from 18 to 30 mg/kg.{48882}
Brand:CaymanSKU:29970 - 5 mgAvailable on backorder
Emetine is an alkaloid that has been found in ipecac root and has diverse biological activities.{53660,31081,36705,53655} It is active against several strains of E. histolytica amoebae (IC50s = 0.73-10.22 μg/ml).{53660} Emetine inhibits NF-κB signaling induced by TNF-α or IL-1β (IC50s = 2 and 4.2 μM, respectively, in a cell-based β-lactamase reporter assay), increases caspase-3/7 activity in ME180 cells (EC50 = 1.1 μM), and is cytotoxic to HeLa cells.{31081} It reduces the infectious virus yield and viral RNA copy numbers in the culture supernatant of Vero E6 cells infected with severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2; EC50s = 0.46 and 0.5 μM, respectively).{53655} Emetine (5 mg/kg) induces emesis in ferrets, an effect that can be prevented by the serotonin (5-HT) receptor subtype 5-HT3 antagonist ondansetron.{36705}
Brand:CaymanSKU:21048 -Out of stock