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CAS No.: 875446-37-0

Anacetrapib/安塞曲匹 Catalog No. CSN12356

Synonyms: MK-0859;安塞曲匹

Anacetrapib is a potent, selective, reversible rhCETP and mutant CETP (C13S) inhibitor with IC50 of 7.9 nM and 11.8 nM, increases HDL-C and decreases LDL-C, does not increase aldosterone or blood pressure.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述Cholesterol ester transfer protein (CETP) is a hydrophobic plasma glycoprotein that has been identified as a promising target for increasing circulating HDL cholesterols. Anacetrapib is an inhibitor of CETP transfer activity, which blocks CETP-dependent transfer of cholesterol esters (CE) with an IC50 value of 17 nM and of triglycerides with an IC50 of 15 nM. When testing the effect of anacetrapib on CE transfer in 95% human serum, the IC50 value was 45 nM when the preincubation time was one hour, and was 18 nM with 24-hour preincubation. Anacetrapib significantly reduced the transfer of CE form HDL3 to HDL2 at a dose-dependent manner from 0.1 to 10 μM in vitro. By adding 25 µM anacetrapib, the amount of [¹⁴C]torcetrapib (0.25 µM) bound to immobilized recombinant human CETP was significantly decreased by 60%. In human plasma with endogenous CETP level at 1.25 μg/ml, incubation of anacetrapib at 0.1, 1, 3, or 10 μM for 21 hours decreased the formation of pre-β—HDL by more than 46%. Hamsters treated with 30 mg/kg anacetrapib once daily for 7 days followed by the injection with [³H]cholesterol-labeled autologous macrophages (Day 0) showed significantly increased level of HDL cholesterol at Day 0, and elevated [³H]cholesterol radioactivity in the HDL fraction at Day 3.
作用机制Anacetrapib inhibits CETP-mediated cholesterol ester and triglyceride transfer by competing with other ligands to reversibly bind to CETP.
动物研究
剂量
Mice: 0.03 mg/kg - 30 mg/kg^[3] (p.o., with diet) Rhesus: 150 mg/kg^[4] (p.o.)

给药途径
p.o.
临床研究

动物研究
剂量	Mice: 0.03 mg/kg - 30 mg/kg^[3] (p.o., with diet) Rhesus: 150 mg/kg^[4] (p.o.)
给药途径	p.o.

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00565006	Ambulatory Blood Pressure	Phase 1	Completed	-	-
NCT00565292	Hypercholesterolemia ... more >> Hyperlipidemia Collapse <<	Phase 1	Completed	-	-
NCT00325455	Hypercholesterolemia ... more >> Mixed Hyperlipemia Collapse <<	Phase 2	Terminated	-	-

更多
参考文献

[1] Ranalletta M, Bierilo KK, et al. Biochemical characterization of cholesteryl ester transfer protein inhibitors. J Lipid Res. 2010;51(9):2739-52.
[2] Niesor EJ, Magg C, et al. Modulating cholesteryl ester transfer protein activity maintains efficient pre-β-HDL formation and increases reverse cholesterol transport. J Lipid Res. 2010;51(12):3443-54.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.5686 mL
- 7.8430 mL
- 15.6860 mL
- 5 mM
- 0.3137 mL
- 1.5686 mL
- 3.1372 mL
- 10 mM
- 0.1569 mL
- 0.7843 mL
- 1.5686 mL

技术信息

CAS号

875446-37-0

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C30H25F10NO3

运输

蓝冰

分子量

637.51

别名

MK-0859;安塞曲匹

溶解度

DMSO	127.0 mg/mL (199.2 mM)
Water	Insoluble
Ethanol	126.0 mg/mL (197.6 mM)

动物实验配方

30% PEG400+0.5% Tween80+5% propylene glycol+water

10 mg/mL

suspension

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NCT00565006	Ambulatory Blood Pressure	Phase 1	Completed	-	-
NCT00565292	Hypercholesterolemia ... more >> Hyperlipidemia Collapse <<	Phase 1	Completed	-	-
NCT00325455	Hypercholesterolemia ... more >> Mixed Hyperlipemia Collapse <<	Phase 2	Terminated	-	-
NCT00977288	Dyslipidemia	Phase 2	Completed	-	-
NCT00990808	Dyslipidemia	Phase 1	Completed	-	-
NCT00685776	Coronary Heart Disease (CHD) ... more >> CHD Risk-Equivalent Disease Collapse <<	Phase 3	Completed	-	-
NCT02931188	-	-	Completed	-	United Kingdom ... more >> Clinical Investigation Ward, Addenbrooke's Hospital Cambridge, Cambridgeshire, United Kingdom, CB2 0QQ Collapse <<
NCT01524289	Hyperlipoproteinemia Type II ... more >> Heterozygous Familial Hypercholesterolemia Collapse <<	Phase 3	Active, not recruiting	November 30, 2018	-
NCT01114490	Dyslipidemia	Phase 1	Completed	-	-
NCT01717300	Hypercholesterolemia	Phase 3	Completed	-	-
NCT01252953	Atherosclerotic Cardiovascular... more >> Disease Collapse <<	Phase 3	Active, not recruiting	April 2019	United Kingdom ... more >> CTSU, University of Oxford Oxford, Oxfordshire, United Kingdom, OX3 7LF Collapse <<
NCT01760460	Dyslipidemia	Phase 3	Completed	-	-
NCT01860729	Hypercholesterolemia	Phase 3	Completed	-	-
NCT01252953	-	-	Active, not recruiting	-	-
NCT01122667	Dyslipidemia	Phase 1	Completed	-	-
NCT01841684	Hyperlipoproteinemia Type II ... more >> Homozygous Familial Hypercholesterolemia Collapse <<	Phase 3	Terminated	-	-
NCT01824238	Heterozygous Familial Hypercho... more >>lesterolemia (HeFH) Collapse <<	Phase 3	Completed	-	-

Anacetrapib/安塞曲匹 Catalog No. CSN12356

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