LY2608204|cas 1234703-40-2|DC Chemicals

Cas No.:	1234703-40-2
Chemical Name:	LY-2608204
Synonyms:	LY2608204;(1R,2S)-2-cyclohexyl-1-(4-cyclopropylsulfonylphenyl)-N-[5-(2-pyrrolidin-1-ylethylsulfanyl)-1,3-thiazol-2-yl]cyclopropane-1-carboxamide;LY-2608204;(1R,2S)-2-Cyclohexyl-1-[4-(cyclopropylsulfonyl)phenyl]-N-[5-[[2-(1-pyrrolidinyl)ethyl]thio]-2-thiazolyl]cyclopropanecarboxamide;Globalagliatin
SMILES:	C1CN(CC1)CCSC2SC(=NC=2)NC(=O)[C@@]3(C4=CC=C(C=C4)S(=O)(=O)C5CC5)[C@H](C6CCCCC6)C3
Formula:	C₂₈H₃₇N₃O₃S₃
M.Wt:	559.802
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

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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