所有图片(1)
别名:
CI-1011; PD 148515; [[2,4,6-三(1-甲基乙基)苯基]乙酰基]-, 2,6-双(1-甲基乙基)苯基酯]氨基磺酸
经验公式（希尔记法）:
C29H43NO4S
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质量水平
检测方案
≥98% (HPLC)
形式
powder
颜色
white to tan
溶解性
DMSO: ≥40 mg/mL
相关疾病
Alzheimer′s disease; cardiovascular diseases
储存温度
room temp
SMILES字符串
CC(C)c1cc(C(C)C)c(CC(=O)NS(=O)(=O)Oc2c(cccc2C(C)C)C(C)C)c(c1)C(C)C
InChI
1S/C29H43NO4S/c1-17(2)22-14-25(20(7)8)27(26(15-22)21(9)10)16-28(31)30-35(32,33)34-29-23(18(3)4)12-11-13-24(29)19(5)6/h11-15,17-21H,16H2,1-10H3,(H,30,31)
InChI key
PTQXTEKSNBVPQJ-UHFFFAOYSA-N
应用
阿伐麦布已被用作Huh7.5.1细胞中酰基辅酶A：胆固醇酰基转移酶（ACAT）的抑制剂，以测试其与直接作用抗病毒药物（DAA）的组合效果，以及其对适应酸中毒的癌细胞中脂质滴积累的影响。它可以用作ACAT的抑制剂来评估克氏锥虫中胆固醇的酯化。
生化/生理作用
阿伐麦布（CI-1011）是一种口服生物可利用的Acyl-CoA:胆固醇O-酰基转移酶（ACAT）抑制剂。它最初作为一种抗惊厥药物被开发，并且被证明能够显著降低血浆总甘油三酯和VLDL-胆固醇，但后来的临床试验令人失望。ACAT也被作为阿尔茨海默病的潜在治疗靶点进行了研究。最近已经研究了阿伐麦布通过限制可扩散淀粉样蛋白-β（Abeta）的产生和增加清除来削弱淀粉样蛋白病变的作用。
法律信息
根据辉瑞公司的协议出售，用于研究目的。
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
Jasminder Sahi et al.
Drug metabolism and disposition: the biological fate of chemicals, 32(12), 1370-1376 (2004-08-31)
Avasimibe, an acyl-CoA:cholesterol acyltransferase inhibitor, has been previously shown to be a potent inducer of CYP3A4 and multiple drug resistance protein 1. We have further characterized the drug interaction potential of avasimibe by studying the inductive and inhibitory effect of
Frederick J Raal et al.
Atherosclerosis, 171(2), 273-279 (2003-12-04)
This study assessed the efficacy and safety of avasimibe (CI-1011), an inhibitor of acyl coenzyme A-cholesterol acyltransferase (ACAT) in subjects with homozygous familial hypercholesterolemia (HoFH). Twenty seven subjects were enrolled in a double-blind, randomized, 3-sequence crossover trial of atorvastatin 80
William R Hiatt et al.
Vascular medicine (London, England), 9(4), 271-277 (2005-02-01)
This study tested the hypothesis that avasimibe, an inhibitor of acyl coenzyme A-cholesterol acyltransferase (ACAT), would improve treadmill exercise performance in patients with claudication secondary to peripheral arterial disease (PAD). Four hundred and forty-two patients with PAD (ankle-brachial index in
Jean-Claude Tardif et al.
Circulation, 110(21), 3372-3377 (2004-11-10)
Inhibition of the acyl coenzyme A:cholesterol acyltransferase (ACAT) enzyme may prevent excess accumulation of cholesteryl esters in macrophages. The ACAT inhibitor avasimibe was shown to reduce experimental atherosclerosis. This study was designed to investigate the effects of avasimibe on human
Yves Rival et al.
DNA and cell biology, 23(5), 283-292 (2004-06-01)
It is now recognized that atherosclerosis complications are related to the unstable character of the plaque rather than its volume. Vulnerable plaques often contain a large lipid core, a reduced content of smooth muscle cells, and accumulation of inflammatory cells.
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