GPR40 Agonist III-Calbiochem

半岛bd体育手机客户端 说明

一般描述

A cell-permeable, orally bioavailable, non-toxic, alkyne derivative that acts as a highly potent, and selective agonist of free fatty acid receptor 1 (FFA1; GPR40; EC₅₀= 20 nM in FFA1-transfected HEK-293 cells). Exhibits lower lipophilicity and excellent metabolic stability. Demonstrates over 100-fold greater selectivity over GPR43, GPR41, GPR120, PPARγ and 55 other receptors, transporters, and enzymes. Improves glucose tolerance in type 2 diabetic mice (~50 mg/kg) with efficacy comparable to DPPIV inhibitor, sitagliptin (~10 mg/kg). Displays favorable pharmacokinetic properties with t 1/2= 17 min and Cmax of 5071 (ng/ml).
A cell-permeable, orally bioavailable, non-toxic, alkyne derivative that acts as a highly potent, and selective agonist of free fatty acid receptor 1 (FFA1; GPR40; EC₅₀= 20 nM in FFA1-transfected HEK-293 cells). Exhibits lower lipophilicity and excellent metabolic stability. Demonstrates over 100-fold greater selectivity over GPR43, GPR41, GPR120, PPARγ and 55 other receptors, transporters, and enzymes. Improves glucose tolerance in type 2 diabetic mice (~50 mg/kg) with efficacy comparable to DPPIV inhibitor, sitagliptin (~10 mg/kg). Displays favorable pharmacokinetic properties with t 1/2= 17 min and Cmax of 5071 (ng/ml).

Please note that the molecular weight for this compound is batch-specific due to variable water content.

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

其他说明

Christiansen, E., et al. 2013.J. Med. Chem.56,982.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

基本信息

经验(实验)分子式	C19H15NO2
分子量	289.33

半岛bd体育手机客户端 性质

质量水平	100
测定	≥98% (HPLC)
形式	powder
manufacturer/tradename	Calbiochem?
储存条件	OK to freeze protect from light
颜色	off-white
溶解性	DMSO: 100 mg/mL
储存温度	2-8℃

安全信息

储存分类代码	11 - Combustible Solids
WGK	WGK 3
闪点(F)	Not applicable
闪点(C)	Not applicable