Evacetrapib is a potent and selective ofCETPinhibitor, which inhibits human recombinantCETPprotein (IC₅₀5.5 nM) andCETPactivity in human plasma (IC₅₀36 nM) in vitro.

IC50: 5.5 nM (CETP)^[1]

Evacetrapib is a novel benzazepine-based CETP inhibitor. In the buffer CETP assay, the absolute potency of the compound is 5.5 nM. In the human plasma CETP assay, the CETP concentration is about 2 μg/mL (25 nM) and the 36 nM IC₅₀value again indicates that Evacetrapib is a potent CETP inhibitor against either the recombinant protein or CETP from human plasma. Evacetrapib is apparently much more potent than Dalcetrapib^[1].

In double transgenic mice expressing human CETP and apoAI, Evacetrapib exhibits an ex vivo CETP inhibition ED₅₀of less than 5 mg/kg at 8 h post oral dose and significantly elevated HDL cholesterol. Importantly, no blood pressure elevation is observed in rats dosed with Evacetrapib at high exposure multiples compared with the positive control, torcetrapib. Evacetrapib administered orally at 30 mg/kg results in 98.4%, 98.6%, and 18.4% inhibition of CETP activity at 4, 8 and 24 h post dose respectively. Evacetrapib dosed orally at 30 mg/kg resulted in 129.7% increase in HDL-C 8 h after oral administration^[1].

638.65

Solid

C₃₁H₃₆F₆N₆O₂

1186486-62-3

Room temperature in continental US; may vary elsewhere.

DMSO : ≥ 100 mg/mL(156.58 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    40%PEG300   5%Tween-80   45% saline

  Solubility: ≥ 2.5 mg/mL (3.91 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (3.91 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH2O 中，得到澄清透明的生理盐水溶液
• 2.

  请依序添加每种溶剂： 10% DMSO    90%corn oil

  Solubility: ≥ 2.5 mg/mL (3.91 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (3.91 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。