166518-60-1

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