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

IC50: 7.9±2.5 nM (rhCETP), 11.8±1.9 nM (CETP^C13S)^[1]

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].

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 (C_max) ranges from 5 to 26 μM and the time to reach peak plasma level (T_max) ranged from 3 to 4.5 h^[3].

637.51

Solid

C₃₀H₂₅F₁₀NO₃

875446-37-0

安塞曲匹；安塞曲比；安塞曲贝

Room temperature in continental US; may vary elsewhere.

DMSO : ≥ 100 mg/mL(156.86 mM)

*"≥" means soluble, but saturation unknown.

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。

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。