959122-11-3A922500

产品属性：

Cas No.959122-11-3

别名 A-922500, A 922500

化学名 (1R,2R)-2-[4-[4-(phenylcarbamoylamino)phenyl]benzoyl]cyclopentane-1-carboxylic acid

分子式 C26H24N2O4

分子量 428.48

溶解度 ≥ 21.25mg/mL in DMSO

储存条件 Store at -20°C
General tips  For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition     Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述：
A922500 is a potent, active, selective and orally bioavailable inhibitor of diacylglycerol acyltransferase-1 (DGAT-1). It is a small molecular with the formula of C26H24N2O4 and molecular weight of 428.48. A922500 inhibits human DGAT-1 with an IC50 value of 9 nM, but does not inhibit other acyltransferases, such as DGAT-2, ACAT-1 and ACAT-2. [1] Diacylglycerol acyltransferase (DGAT) catalyzes esteri?cation of 1,2-diacylglycerol (DAG) with fatty acyl-CoA to form triglycerides (TG) at the endoplasmic reticulum.[2]

Reference

[1] Andrew J. K, Jason A. S, Kelly J. L, Andrew J. S, Philip R. K, Regina M. R, et al. In vivo efficacy of acyl CoA: Diacylglycerol acyltransferase (DGAT) 1 inhibition in rodent models of postprandial hyperlipidemia. European Journal of Pharmacology. 2010, 637. 155-161.

[2] Kyeong L, Ja-Il G,  Hwa Young J, Minkyoung K, Shanthaveerappa K. B, et al. Discovery of a novel series of benzimidazole derivatives as diacylglycerol acyltransferase inhibitors. Bioorganic & Medicinal Chemistry Letters. 2012, 22. 7456–7460.