化学名称 : 阿伐麦布
CAS : 166518-60-1
英文名称: Avasimibe(CI-1011)/
英文同义词: AVASIMIBE
溶解度:Unknown
储存条件:at -20℃ 2 years
生物活性
Avasimibe(CI-1011) is a novel orally bioavailable acyl coenzyme A:cholesterol acyltransferase inhibitor with IC50 of 2.9, 13.9, 26.5 µM for CYP2C9, CYP1A2, and CYP2C19.
Avasimibe(CI-1011) has been previously shown to be a potent inducer of CYP3A4 and multiple drug resistance protein 1. [1] In a study, avasimibe decreased the VLDL apoB pool size by 40–43% and the hepatic secretion rate of VLDL apoB by 38–41%, but did not alter its fractional catabolism. Avasimibe decreased the LDL apoB pool size by 13–57%, largely due to a dose-dependent 25–63% in the LDL apoB production rate. Hepatic LDL receptor mRNA abundances were unchanged, consistent with a marginal decrease in LDL apoB FCRs. Hepatic ACAT activity was decreased by 51% (P = 0.050) and 68% (P = 0.087) by low and high dose avasimibe, respectively.
参考文献
[1] Sahi J et al. Drug Metab Dispos. 2004 Dec;32(12):1370-6.
[2] Burnett JR et al. J Lipid Res. 1999 Jul;40(7):1317-27.
[3] http://www.ncbi.nlm.nih.gov/pubmed/12595916