Pactimibe (CS-505 free base) is a dualACAT1/2inhibitor withIC₅₀s of 4.9 μM and 3.0 μM, respectively. Pactimibe (CS-505 free base) inhibitsACATwithIC₅₀s of 2.0 μM, 2.7 μM, 4.7 μM in the liver, macrophages and THP-1 cells, respectively^[1]. Pactimibe (CS-505 free base) noncompetitively inhibitsoleoyl-CoAwith aK_ivalue of 5.6 μM. Moreover, Pactimibe (CS-505 free base) obviously inhibitscholesteryl ester formationwith anIC₅₀of 6.7 μM. Pactimibe (CS-505 free base) possesses anti-atherosclerotic potential with lowering plasmacholesterolactivity^[2].

Pactimibe (CS-505 free base) induces moderate ACAT inhibition in monocyte-derived macrophages, leading to the suppression of foam cell formation^[2].

Pactimibe (CS-505 free base; 60 and 200 mg/kg/day; oral gavage; twice a day; 12 weeks) induces an inhibition for ACAT-1 and ACAT-2, causing a reduction of plasma cholesterol but no influence on macrophage- or collagen-positive areas^[3].

416.60

Solid

C₂₅H₄₀N₂O₃

189198-30-9

帕替麦布

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

DMSO : 200 mg/mL(480.08 mM;Need ultrasonic)

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 (sealed storage, away from moisture)。-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: ≥ 5 mg/mL (12.00 mM); Clear solution

  此方案可获得 ≥ 5 mg/mL (12.00 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 50.0 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