1234703-40-2

1234703-40-2 structure

Name: LY2608204
Chemical Name: (1R,2S)-2-cyclohexyl-1-(4-cyclopropylsulfonylphenyl)-N-[5-(2-pyrrolidin-1-ylethylsulfanyl)-1,3-thiazol-2-yl]cyclopropane-1-carboxamide
CAS Number: 1234703-40-2
Molecular Formula: C₂₈H₃₇N₃O₃S₃
Molecular Weight: 559.807
Catalog: Signaling Pathways Metabolic Enzyme/Protease Glucokinase
Create Date: 2018-12-30 12:11:13
Modify Date: 2024-01-08 10:25:39
LY2608204 is a activator of glucokinase (GK) with EC50 of 42 nM.IC 50 value: 42 nM (EC50)Target: glucokinasein vitro: LY2608204 activates glucokinase (GK) with EC50 of 42 nM at 10 mM glucose with a concentration dependent manner at lower glucose concentrations. LY2608204 also stimulates glucose metabolism in rat insulinoma INS1-E cells with EC50 of 579 nM.in vivo: LY2608204 decreases plasma glucose in a dose-dependent manner at both fasted and postprandial glucose levels. A maximal lowering of glucose AUC versus the untreated control group is observed with the high dose (30 mg/kg) and represents a 42% decrease. Interpolation of the data show that a 20% glucose AUC decrease occurs at an average LY2608204 concentration of 99 ng/mL (179 nM) in plasma, corresponding to a 6.9 mg/kg LY2608204 dose. The in vivo blood brain barrier permeability of LY2608204 results in a mean brain/plasma ratio of 0.17 five minutes post-dose with a mean total brain level of 0.539 nmol/g.Clinical trail:

Name	(1R,2S)-2-cyclohexyl-1-(4-cyclopropylsulfonylphenyl)-N-[5-(2-pyrrolidin-1-ylethylsulfanyl)-1,3-thiazol-2-yl]cyclopropane-1-carboxamide
Synonyms	(1R,2S)-2-cyclohexyl-1-[4-(cyclopropanesulfonyl)phenyl]-N-(5-{[2-(pyrrolidin-1-yl)ethyl]sulfanyl}-1,3-thiazol-2-yl)cyclopropane-1-carboxamide (1R,2S)-2-cyclohexyl-1-(4-cyclopropanesulfonylphenyl)cyclopropanecarboxylic acid [5-(2-pyrrolidin-1-ylethylsulfanyl)thiazol-2-yl]amide (1R,2S)-2-Cyclohexyl-1-[4-(cyclopropylsulfonyl)phenyl]-N-(5-{[2-(1-pyrrolidinyl)ethyl]sulfanyl}-1,3-thiazol-2-yl)cyclopropanecarboxamide Cyclopropanecarboxamide, 2-cyclohexyl-1-[4-(cyclopropylsulfonyl)phenyl]-N-[5-[[2-(1-pyrrolidinyl)ethyl]thio]-2-thiazolyl]-, (1R,2S)- LY2608204

Description	LY2608204 is a activator of glucokinase (GK) with EC50 of 42 nM.IC 50 value: 42 nM (EC50)Target: glucokinasein vitro: LY2608204 activates glucokinase (GK) with EC50 of 42 nM at 10 mM glucose with a concentration dependent manner at lower glucose concentrations. LY2608204 also stimulates glucose metabolism in rat insulinoma INS1-E cells with EC50 of 579 nM.in vivo: LY2608204 decreases plasma glucose in a dose-dependent manner at both fasted and postprandial glucose levels. A maximal lowering of glucose AUC versus the untreated control group is observed with the high dose (30 mg/kg) and represents a 42% decrease. Interpolation of the data show that a 20% glucose AUC decrease occurs at an average LY2608204 concentration of 99 ng/mL (179 nM) in plasma, corresponding to a 6.9 mg/kg LY2608204 dose. The in vivo blood brain barrier permeability of LY2608204 results in a mean brain/plasma ratio of 0.17 five minutes post-dose with a mean total brain level of 0.539 nmol/g.Clinical trail:
Related Catalog	Signaling Pathways >> Metabolic Enzyme/Protease >> Glucokinase Research Areas >> Metabolic Disease

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