LY2608204 structure
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Common Name | LY2608204 | ||
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CAS Number | 1234703-40-2 | Molecular Weight | 559.807 | |
Density | 1.4±0.1 g/cm3 | Boiling Point | N/A | |
Molecular Formula | C28H37N3O3S3 | Melting Point | N/A | |
MSDS | N/A | Flash Point | N/A |
Use of LY2608204LY2608204 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 |
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Synonym | More Synonyms |
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: |
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Related Catalog |
Density | 1.4±0.1 g/cm3 |
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Molecular Formula | C28H37N3O3S3 |
Molecular Weight | 559.807 |
Exact Mass | 559.199707 |
PSA | 144.78000 |
LogP | 4.97 |
Index of Refraction | 1.658 |
Hazard Codes | Xi |
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(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 |