Pactimibe sulfate

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Pactimibe sulfate

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CAS NO:

608510-47-0

包装与价格：

包装	价格(元)
10mM (in 1mL DMSO)	询价
5mg	询价
10mg	询价
25mg	询价
50mg	询价
100mg	询价

Pactimibe sulfate (CS-505) 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 sulfate (CS-505) 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 sulfate (CS-505) 非竞争性抑制 oleoyl-CoA，Ki 是5.6 µM。此外，Pactimibe sulfate (CS-505) 明显抑制胆固醇酯的形成，IC50 是6.7 µM。Pactimibe sulfate (CS-505) 具有抗动脉粥样硬化的潜力，可降低血浆胆固醇的活性。

Cas No.	608510-47-0
别名	帕替麦布,CS-505
Canonical SMILES	O=C(O)CC1=C(C)C2=C(N(CCCCCCCC)CC2)C(NC(C(C)(C)C)=O)=C1C.O=S(O)(O)=O.[1/2]
分子式	C₂₅H₄₀N₂O₃.₁/₂H₂O₄S
分子量	465.65
溶解度	DMSO : 120 mg/mL (257.70 mM)
储存条件	4℃, away from moisture
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
产品描述	Pactimibe sulfate (CS-505) is a dual ACAT1/2 inhibitor with IC50s of 4.9 µM and 3.0 µM, respectively. Pactimibe sulfate (CS-505) 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 sulfate (CS-505) noncompetitively inhibits oleoyl-CoA with a Ki value of 5.6 µM. Moreover, Pactimibe sulfate (CS-505) obviously inhibits cholesteryl ester formation with an IC50 of 6.7 µM. Pactimibe sulfate (CS-505) possesses anti-atherosclerotic potential with lowering plasma cholesterol activity[2]. Pactimibe sulfate (CS-505) induces moderate ACAT inhibition in monocyte-derived macrophages, leading to the suppression of foam cell formation[2]. Pactimibe sulfate (CS-505; 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]. References: [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.