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Anacetrapib
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Anacetrapib图片
CAS NO:875446-37-0
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品名称
安塞曲匹
MK-0859
产品介绍
Anacetrapib 是一种有效的CETP抑制剂,作用于 rhCETP 和 C13S CETP 突变型,IC50分别为 7.9±2.5 nM 和 11.8±1.9 nM。
生物活性

Anacetrapib is a potentCETPinhibitor, withIC50s of 7.9±2.5 nM and 11.8±1.9 nM for rhCETP and C13SCETPmutant, respectively.

IC50& Target

IC50: 7.9±2.5 nM (rhCETP), 11.8±1.9 nM (CETPC13S)[1]

体外研究
(In Vitro)

Anacetrapib dose-dependently and significantly decreases the transfer of CE from HDL3 to HDL2 (P<0.001 for concentrations equal to and higher than 0.1 μM). Excess Anacetrapib (25 μM) decreases the amount of [14C]Torcetrapib (0.25 μM) binds to immobilized rhCETP by 82% and 60%, respectively. Anacetrapib decreases pre-β-HDL formation by more than 46% (P<0.001) at all concentrations tested (0.1, 1, 3, and 10 μM)[1]. A significant reduction of PCSK9 promoter activity by Anacetrapib (ANA) is detected at 3 μM concentration (–22%, p<0.01) and further lowered to 68% of control at 10 μM. Likewise, luciferase activity of B11 cells are decreased by Anacetrapib at 3 μM concentration and reached to a maximal reduction of 38% of control at 10 μM. At 10 μM concentration, Anacetrapib loweres PCSK9 mRNA level to 60% of control and LDLR mRNA level to 67% of control[2].

体内研究
(In Vivo)

Hamsters are given Anacetrapib for 7 days before injection of [3H]cholesterol-labeled macrophages (day 0). Treatment with Anacetrapib leads to significant increases in HDL-C levels at day 0. At day 3, [3H]cholesterol radioactivity in the HDL fraction is significantly increased from control values for Anacetrapib[1]. Anacetrapib (ANA) treatment modestly elevates serum total serum cholesterol levels ~10% (p<0.05) and increases serum LDL-C by 26% (p<0.05) as compared to vehicle control[2]. After an intravenous dose of 0.5 mg/kg, the mean values for systemic plasma clearance, steady-state volume of distribution, and terminal half-life are 2.3 mL/min/kg, 1.1 L/kg, and 12 h, respectively. After oral dosing at 5 mg/kg, the bioavailability of Anacetrapib is 38%. Exposures (AUC) increases in a less than dose-proportional manner from 23 μMoh at 5 mg/kg to 362 μMoh at 500 mg/kg. In this dose range, the peak plasma level (Cmax) ranges from 5 to 26 μM and the time to reach peak plasma level (Tmax) ranged from 3 to 4.5 h[3].

Clinical Trial
分子量

637.51

性状

Solid

Formula

C30H25F10NO3

CAS 号

875446-37-0

中文名称

安塞曲匹;安塞曲比;安塞曲贝

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : ≥ 100 mg/mL(156.86 mM)

*"≥" means soluble, but saturation unknown.

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.5686 mL7.8430 mL15.6860 mL
5 mM0.3137 mL1.5686 mL3.1372 mL
10 mM0.1569 mL0.7843 mL1.5686 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

    Solubility: ≥ 2.75 mg/mL (4.31 mM); Clear solution

    此方案可获得 ≥ 2.75 mg/mL (4.31 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 27.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在本网站选购。