Pactimibe帕替麦布,189198-30-9

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Pactimibe

CAS No. : 189198-30-9

MCE 国际站：Pactimibe

产品活性：Pactimibe (CS-505 free base) 是一种 ACAT1/2 双重抑制剂，对于 ACAT1 的 IC₅₀ 值为 4.9 μM，对于 ACAT2 的 IC₅₀ 值为 3.0 μM。Pactimibe (CS-505 free base) 抑制 ACAT，其 IC₅₀ 值在肝细胞中是 2.0 μM，在巨噬细胞中是 2.7 μM，在 THP-1 细胞中是 4.7 μM。Pactimibe (CS-505 free base) 非竞争性抑制 oleoyl-CoA，K_i 是5.6 μM。此外，Pactimibe (CS-505 free base) 明显抑制胆固醇酯的形成，IC₅₀ 是6.7 μM。Pactimibe (CS-505 free base) 具有抗动脉粥样硬化的潜力，可降低血浆胆固醇的活性。

研究领域：Metabolic Enzyme/Protease

作用靶点：Acyltransferase

In Vitro: Pactimibe (CS-505 free base) induces moderate ACAT inhibition in monocyte-derived macrophages, leading to the suppression of foam cell formation.

In Vivo: 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.

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