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阿伐麦布

阿伐麦布用途

Avasimibe是一种可口服的酰基辅酶A: 胆固醇酰基转移酶 (ACAT) 抑制剂,IC50 分别为24 和 9.2 µM。

阿伐麦布名称

[ CAS 号 ]:
166518-60-1

[ 中文名 ]:
阿伐麦布

[ 英文名 ]:
Avasimibe

[中文别名 ]:

[英文别名 ]:

Avasimibe
CI-1011

阿伐麦布生物活性

[ 描述 ]:

Avasimibe是一种可口服的酰基辅酶A: 胆固醇酰基转移酶 (ACAT) 抑制剂,IC50 分别为24 和 9.2 µM。

[ 相关类别 ]:

信号通路 >> 代谢酶/蛋白酶 >> 酰基转移酶

研究领域 >> 癌症

[参考文献]

[1]. Tardif JC et al. Effects of the acyl coenzyme A:cholesterol acyltransferase inhibitor avasimibe on human atherosclerotic lesions. Circulation, 2004 Nov 23, 110(21):3372-7.

[2]. Raal FJ et al. Avasimibe, an ACAT inhibitor, enhances the lipid lowering effect of atorvastatin in subjects with homozygousfamilial hypercholesterolemia. Atherosclerosis, 2003 Dec, 171(2):273-9.

[3]. Delsing DJ et al. Acyl-CoA:cholesterol acyltransferase inhibitor avasimibe reduces atherosclerosis in addition to its cholesterol-lowering effect in ApoE*3-Leiden mice. Circulation, 2001 Apr 3, 103(13):1778-86.

[相关活性小分子]

阿伐麦布物理化学性质

[ 密度 ]:
1.1±0.1 g/cm3

[ 熔点 ]:
178-180° (Lee); mp 169.5-170.4° (Dozeman)

[ 分子式 ]:
C₂₉H₄₃NO₄S

[ 分子量 ]:
501.721

[ 精确质量 ]:
501.291290

[ PSA ]:
80.85000

[ LogP ]:
9.34

[ 外观性状 ]:
white to tan

[ 折射率 ]:
1.529

[ 储存条件 ]:
room temp

[ 水溶解性 ]:
DMSO: ≥40mg/mL

阿伐麦布MSDS

阿伐麦布毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: CY1482550

CHEMICAL NAME :: Benzeneacetamide, N-((2,6-bis(1-methylethyl)phenoxy)sulfonyl)-2,4,6-tri s(1-methylethyl)-

CAS REGISTRY NUMBER :: 166518-60-1

LAST UPDATED :: 199712

DATA ITEMS CITED :: 1

MOLECULAR FORMULA :: C29-H43-N-O4-S

MOLECULAR WEIGHT :: 501.79

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 137 gm/kg/13W-C

TOXIC EFFECTS :: Behavioral - food intake (animal) Skin and Appendages - hair Nutritional and Gross Metabolic - weight loss or decreased weight gain

REFERENCE :: FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year: 36(1, Pt 2),274,1997

阿伐麦布安全信息

[ 危险品运输编码 ]:
NONH for all modes of transport

[ 海关编码 ]:
2935009090

阿伐麦布合成路线

阿伐麦布上下游产品

阿伐麦布上游产品

阿伐麦布下游产品

阿伐麦布海关

[ 海关编码 ]: 2935009090

[ 中文概述 ]:
2935009090 其他磺（酰）胺. 增值税率:17.0% 退税率:9.0% 监管条件:无最惠国关税:6.5% 普通关税:35.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2935009090 other sulphonamides VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:35.0%

阿伐麦布文献

Statin therapy alone and in combination with an acyl-CoA:cholesterol O-acyltransferase inhibitor on experimental atherosclerosis.

Pathophysiol. Haemost. Thromb. 36(1) , 9-17, (2007)

The ability to modify the enzymatic processes involved in promoting atherosclerotic plaque disruption and to serially monitor atherosclerotic evolution could provide novel information in the managemen...

Coronary circulatory function in patients with the metabolic syndrome.

J. Nucl. Med. 52(9) , 1369-77, (2011)

The metabolic syndrome affects 25% of the U.S. population and greatly increases the risk of diabetes and coronary artery disease (CAD). We tested the hypothesis that the metabolic syndrome is associat...

Avasimibe and atorvastatin synergistically reduce cholesteryl ester content in THP-1 macrophages.

Eur. J. Pharmacol. 451(1) , 11-7, (2002)

Evidence suggests that the inhibition of both acyl-CoA:cholesterol acyltransferase and hydroxymethyl glutaryl-CoA reductase causes a synergistic direct antiatherosclerotic effect on the vessel wall. T...

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