608510-47-0

608510-47-0 structure

Name: Pactimibe sulfate
Chemical Name: 2-[7-(2,2-dimethylpropanoylamino)-4,6-dimethyl-1-octyl-2,3-dihydroindol-5-yl]acetic acid,sulfuric acid
CAS Number: 608510-47-0
Molecular Formula: C₅₀H₈₂N₄O₁₀S
Molecular Weight: 931.27200
Catalog: Research Areas Cardiovascular Disease
Create Date: 2017-04-24 11:19:22
Modify Date: 2024-01-10 12:25:54
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].

Name	2-[7-(2,2-dimethylpropanoylamino)-4,6-dimethyl-1-octyl-2,3-dihydroindol-5-yl]acetic acid,sulfuric acid
Synonyms	1H-Indole-5-acetic acid,7-((2,2-dimethyl-1-oxopropyl)amino)-2,3-dihydro-4,6-dimethyl-1-octyl-,sulfate (2:1) CS-505 Pactimibe sulfate UNII-FX3YKK43YM

Description	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].
Related Catalog	Research Areas >> Cardiovascular Disease
Target	ACAT1:4.9 μM (IC50) ACAT2:3.0 μM (IC50) ACAT:2 μM (IC50, in the liver) ACAT:2.7 μM (IC50, in macrophages) ACAT:4.7 μM (IC50, in THP-1 cells) oleoyl-CoA:5.6 μM (Ki) cholesteryl ester formation:6.7 μM (IC50)
In Vitro	Pactimibe sulfate (CS-505) induces moderate ACAT inhibition in monocyte-derived macrophages, leading to the suppression of foam cell formation[2].
In Vivo	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]. Animal Model: Male C57BL/6J ApoE−/− mice aged 8-week-old[3] Dosage: 60 and 200 mg/kg/day Administration: Oral gavage; twice a day; 12 weeks Result: Decreased plasma cholesterol levels by 39% and 74% at the administration of 60 and 200 mg/kg/day.
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.

Molecular Formula	C₅₀H₈₂N₄O₁₀S
Molecular Weight	931.27200
Exact Mass	930.57500
PSA	229.24000
LogP	13.13320

Hazard Codes	Xi

608510-47-0	189198-30-9
60585-57-1	1228182-35-1
10333-92-3	87587-61-9
20997-99-3	63653-42-9
65-30-5	7446-18-6