acat-in-5

ACAT-IN-5 (example 19) is a compound that functions as an inhibitor of acyl-Coenzyme A: cholesterol acyltransferase (ACAT). By inhibiting ACAT, this compound effectively suppresses the transcription mediated by NF-κB.

TMP-153 是一种新型高效的 ACAT 抑制剂，对动物肠道和肝脏 ACAT 的 IC50 值为 5-10 nM。TMP-153  具有降胆固醇作用，可抑制大鼠和仓鼠的胆固醇吸收并降低血浆胆固醇。

Phenylpyropene A is a fungal metabolite originally isolated from P. griseofulvum that has enzyme inhibitory and insecticidal activities.1,2,3 It inhibits acyl-coenzyme A:cholesterol acyltransferase (ACAT; IC50 = 0.8 μM).1 Phenylpyropene A inhibits diacylglycerol acyltransferase (DGAT) in rat liver microsomes (IC50 = 78.7 μM). It induces mortality in 100% of M. persicae when used at a concentration of 5 ppm.3 |1. Kwon, O.E., Rho, M.C., Song, H.Y., et al. Phenylpyropene A and B, new inhibitors of acyl-CoA: Cholesterol acyltransferase produced by Penicillium griseofulvum F1959. J. Antibiot. (Tokyo) 55(11), 1004-1008 (2002).|2. Lee, S.W., Rho, M.C., Choi, J.H., et al. Inhibition of diacylglycerol acyltransferase by phenylpyropenes produced by Penicillium griseofulvum F1959. J. Microbiol. Biotechnol. 18(11), 1785-1788 (2008).|3. Horikoshi, R., Goto, K., Mitomi, M., et al. Identification of pyripyropene A as a promising insecticidal compound in a microbial metabolite screening. J. Antibiot. (Tokyo) 70(3), 272-276 (2017).

Glabrol 是分离自甘草根的乙醇提取物中的一种异戊二烯类黄酮，是一种有效且非竞争性的酰基辅酶 A：胆固醇酰基转移酶（ACAT）抑制剂，抑制大鼠肝脏微粒体 ACAT 的IC50为 24.6 μM。