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Merck
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PZ0190

Sigma-Aldrich

阿伐麦布

≥98% (HPLC)

同義詞:

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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About This Item

經驗公式（希爾表示法）:
C29H43NO4S
CAS號碼:
166518-60-1
分子量：:
501.72
MDL號碼:
MFCD00934956
分類程式碼代碼:
12352200
PubChem物質ID:
329823764

化驗

≥98% (HPLC)

形狀

powder

顏色

white to tan

溶解度

DMSO: ≥40 mg/mL

相關疾病

Alzheimer′s disease; cardiovascular diseases

儲存溫度

room temp

SMILES 字串

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 密鑰

PTQXTEKSNBVPQJ-UHFFFAOYSA-N

應用

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。

法律資訊

根据辉瑞公司的协议出售，用于研究目的。

儲存類別代碼

11 - Combustible Solids

水污染物質分類（WGK）

WGK 3

閃點（°F）

Not applicable

閃點（°C）

Not applicable

分析證明 (COA)

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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.
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
John R Burnett et al.
Current opinion in investigational drugs (London, England : 2000), 3(9), 1328-1333 (2002-12-25)
Avasimibe (also known as CI-1011 or PD-148515) is a selective acyl-coenzyme A:cholesterol O-acyltransferase (ACAT) inhibitory lipid-regulating agent under development by Pfizer (formerly Parke-Davis) for the potential treatment of hyperlipidemia and atherosclerosis. The compound is currently undergoing phase III clinical trials
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
Jean-Claude Tardif et al.
The American journal of cardiology, 98(1), 23-27 (2006-06-21)
We assessed vascular changes during atherosclerosis regression. Compensatory enlargement of coronary arteries accommodates plaque burden during atherosclerosis development. Lipid-lowering therapy has altered the natural history of coronary atherosclerosis, but the arterial changes that occur during disease regression need to be
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