产品说明书

Anacetrapib

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Chemical Structure| 875446-37-0 同义名 : MK-0859
CAS号 : 875446-37-0
货号 : A293882
分子式 : C30H25F10NO3
纯度 : 98%
分子量 : 637.508
MDL号 : MFCD16294903
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(164.7 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

30% PEG400+0.5% Tween80+5% propylene glycol+water 10 mg/mL suspension

生物活性
靶点

  • CETP

    Mutant CETP (C13S), IC50:11.8 nM

    rhCETP, IC50:7.9 nM
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.
临床研究
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 ... 展开 >> Hyperlipidemia 收起 << Phase 1 Completed - -
NCT00325455 Hypercholesterolemia ... 展开 >> Mixed Hyperlipemia 收起 << Phase 2 Terminated - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.57mL

0.31mL

0.16mL

7.84mL

1.57mL

0.78mL

15.69mL

3.14mL

1.57mL
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.