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  • Pactimibe
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Pactimibe

Pactimibe(CS-505freebase)是一种ACAT1/2双重抑制剂,对于ACAT1的IC50值为4.9μM,对于ACAT2的IC50值为3.0μM。Pactimibe(CS-505freebase)抑制ACAT,其IC50值在肝细胞中是2.0μM,在巨噬细胞中是2.7μM,在THP-1细胞中是4.7μM。Pactimibe(CS-505freebase)非竞争性抑制oleoyl-CoA,Ki是5.6μM。此外,Pactimibe(CS-505freebase)明显抑制胆固醇酯的形成,IC50

原价
¥4850-40612
价格
3880-32490
Pactimibe的二维码

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  • 货号: ajcx32144
  • CAS: 189198-30-9
  • 别名: 帕替麦布; CS-505 free base
  • 分子式: C25H40N2O3
  • 分子量: 416.6
  • 纯度: >98%
  • 溶解度: DMSO: 200 mg/mL (480.08 mM)
  • 储存: 4°C, away from moisture
  • 库存: 现货

Background

Pactimibe (CS-505 free base) is a dual ACAT1/2 inhibitor with IC50s of 4.9 μM and 3.0 μM, respectively. Pactimibe (CS-505 free base) inhibits ACAT with IC50s 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 inhibits oleoyl-CoA with a Ki value of 5.6 μM. Moreover, Pactimibe (CS-505 free base) obviously inhibits cholesteryl ester formation with an IC50 of 6.7 μM. Pactimibe (CS-505 free base) possesses anti-atherosclerotic potential with lowering plasma cholesterol activity[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]. Animal Model: Male C57BL/6J ApoE-/- mice aged 8-week-old[3]


[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. [3]. Yasunobu Yoshinaka, et al. A selective ACAT-1 inhibitor, K-604, stimulates collagen production in cultured smooth muscle cells and alters plaque phenotype in apolipoprotein E-knockout mice. Atherosclerosis. 2010 Nov;213(1):85-91.

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