Pactimibe|189198-30-9|(帕替麦布; CS-505 free base)-陌孚医药/Medlife

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Pactimibe (Synonyms: 帕替麦布; CS-505 free base)

目录号: PL14725 纯度: ≥98%

CAS No. :189198-30-9

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中文名称	Pactimibe
中文别名	帕替麦布;7-[(2,2-二甲基-1-氧代丙基)氨基]-2,3-二氢-4,6-二甲基-1-辛基-1H-吲哚-5-乙酸
英文名称	Pactimibe
英文别名	Pactimibe;7-[(2,2-Dimethyl-1-oxopropyl)amino]-2,3-dihydro-4,6-dimethyl-1-octyl-1H-indole-5-acetic acid;2-[7-(2,2-dimethylpropanoylamino)-4,6-dimethyl-1-octyl-2,3-dihydroindol-5-yl]acetic acid;UNII-D874R9PZ9T;PactiMib;2-[7-(2,2-dimethylpropanoylamino)-4,6-dimethyl-1-octyl-2,3-dihydroindo l-5-yl]acetic acid
Cas No.	189198-30-9
分子式	C₂₅H₄₀N₂O₃
分子量	416.60
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情

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。

生物活性

Pactimibe (CS-505 free base) is a dual ACAT1/2 inhibitor with IC 50 s of 4.9 μM and 3.0 μM, respectively. Pactimibe (CS-505 free base) inhibits ACAT with IC 50 s of 2.0 μM, 2.7 μM, 4.7 μM in the liver, macrophages and THP-1 cells, respectively. Pactimibe (CS-505 free base) noncompetitively inhibits oleoyl-CoA with a K i value of 5.6 μM. Moreover, Pactimibe (CS-505 free base) obviously inhibits cholesteryl ester formation with an IC 50 of 6.7 μM. Pactimibe (CS-505 free base) possesses anti-atherosclerotic potential with lowering plasma cholesterol activity.

性状

Solid

IC50 & Target[1][2]

ACAT1 4.9 μM (IC50) ACAT2 3.0 μM (IC5

体外研究(In Vitro)

Pactimibe (CS-505 free base) induces moderate ACAT inhibition in monocyte-derived macrophages, leading to the suppression of foam cell formation. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

参考文献

[1]. Naoki Terasaka, et al. ACAT inhibitor pactimibe sulfate (CS-505) reduces and stabilizes atherosclerotic lesions by cholesterol-lowering and direct effects in apolipoprotein E-deficient mice. Atherosclerosis. 2007 Feb;190(2):239-47.
[2]. Ken Kitayama, et al. Importance of acyl-coenzyme A:cholesterol acyltransferase 1/2 dual inhibition for anti-atherosclerotic potency of pactimibe. Eur J Pharmacol. 2006 Jul 1;540(1-3):121-30.

溶解度数据	In Vitro: DMSO : 200 mg/mL (480.08 mM; Need ultrasonic)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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