CAS NO: | 959122-11-3 |
规格: | 98% |
分子量: | 428.48 |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
200mg | 电议 |
Background:
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 C26H24N2O4and 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.