PZ0190
阿伐麦布
≥98% (HPLC)
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
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关于此项目
经验公式（希尔记法）:
C29H43NO4S
化学文摘社编号:
分子量:
501.72
UNSPSC Code:
12352200
PubChem Substance ID:
MDL number:
NACRES:
NA.28
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)
SMILES string
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 key
PTQXTEKSNBVPQJ-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
powder
color
white to tan
solubility
DMSO: ≥40 mg/mL
relevant disease(s)
Alzheimer′s disease; cardiovascular diseases
storage temp.
room temp
Quality Level
Application
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。
Biochem/physiol Actions
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
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。
存储类别
11 - Combustible Solids
flash_point_f
Not applicable
flash_point_c
Not applicable
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
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
John R Burnett et al.
Biochimica et biophysica acta, 1738(1-3), 10-18 (2006-01-24)
Previously, we have shown, in vivo, that the acyl coenzyme A: cholesterol acyltransferase (ACAT) inhibitor avasimibe decreases hepatic apolipoprotein (apo) B secretion into plasma. To test the hypothesis that avasimibe modulates postprandial triglyceride-rich lipoprotein (TRL) metabolism in vivo, an oral
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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