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托彻普

托彻普用途

Torcetrapib(CP-529414)是CETP高效抑制剂,IC50值为37nM。

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托彻普名称

[ CAS 号 ]:
262352-17-0

[ 中文名 ]:
托彻普

[ 英文名 ]:
Torcetrapib

[中文别名 ]:

[英文别名 ]:

Torcetrapib
MFCD08063631

托彻普生物活性

[ 描述 ]:

Torcetrapib(CP-529414)是CETP高效抑制剂,IC50值为37nM。

[ 相关类别 ]:

信号通路 >> 代谢酶/蛋白酶 >> CETP

研究领域 >> 内分泌

[参考文献]

[1]. Clark RW, et al. Raising high-density lipoprotein in humans through inhibition of cholesteryl ester transfer protein: an initial multidose study of torcetrapib. Arterioscler Thromb Vasc Biol. 2004 Mar;24(3):490-7.

[2]. Hu X, et al. Torcetrapib induces aldosterone and cortisol production by an intracellular calcium-mediated mechanism independently of cholesteryl ester transfer protein inhibition. Endocrinology. 2009 May;150(5):2211-9.

[3]. Barter PJ, et al. Effects of torcetrapib in patients at high risk for coronary events. N Engl J Med. 2007 Nov 22;357(21):2109-22.

[4]. Morehouse LA, et al. Inhibition of CETP activity by torcetrapib reduces susceptibility to diet-induced atherosclerosis in New Zealand White rabbits. J Lipid Res. 2007 Jun;48(6):1263-72.

[相关活性小分子]

安塞曲匹 | CETP抑制剂 | Evacetrapib

托彻普物理化学性质

[ 密度 ]:
1.4±0.1 g/cm3

[ 沸点 ]:
504.8±50.0 °C at 760 mmHg

[ 熔点 ]:
54-58ºC

[ 分子式 ]:
C₂₆H₂₅F₉N₂O₄

[ 分子量 ]:
600.47

[ 闪点 ]:
259.1±30.1 °C

[ PSA ]:
59.08000

[ LogP ]:
7.76

[ 外观性状 ]:
液体

[ 蒸汽压 ]:
0.0±1.3 mmHg at 25°C

[ 折射率 ]:
1.512

[ 储存条件 ]:
Store at RT

托彻普安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302

[ 危害码 (欧洲) ]:
Xn

[ 风险声明 (欧洲) ]:
22

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

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托彻普文献

Cholesteryl ester-transfer protein inhibitors stimulate aldosterone biosynthesis in adipocytes through Nox-dependent processes.

J. Pharmacol. Exp. Ther. 353(1) , 27-34, (2015)

Hyperaldosteronism and hypertension were unexpected side effects observed in trials of torcetrapib, a cholesteryl ester-transfer protein (CETP) inhibitor that increases high-density lipoprotein. Given...

Effect on cardiovascular risk of high density lipoprotein targeted drug treatments niacin, fibrates, and CETP inhibitors: meta-analysis of randomised controlled trials including 117,411 patients.

BMJ 349 , g4379, (2014)

To investigate the effects on cardiovascular outcomes of drug interventions that increase high density lipoprotein levels.Meta-analysis.Therapeutic benefit of niacin, fibrates, and cholesteryl ester t...

Identification of a novel, non-tetrahydroquinoline variant of the cholesteryl ester transfer protein (CETP) inhibitor torcetrapib, with improved aqueous solubility.

Xenobiotica 44(7) , 591-605, (2014)

1. Elaborate studies of cholesteryl ester transfer protein (CETP) polymorphisms and genetic deficiency in humans suggest direct links between CETP, high-density lipoprotein cholesterol (HDL-c) levels ...

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托彻普