Pactimibe (sulfate)
Product Specifications
UNSPSC 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].
Target Antigen
Acyltransferase
Type
Reference compound
Related Pathways
Metabolic Enzyme/Protease
Applications
Neuroscience-Neuromodulation
Field of Research
Cardiovascular Disease
Assay Protocol
https://www.medchemexpress.com/pactimibe-sulfate.html
Purity
98.0
Solubility
DMSO : 120 mg/mL (ultrasonic)|H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C)
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]
Molecular Weight
465.65
References & Citations
[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.
Shipping Conditions
Room Temperature
Storage Conditions
4°C (Powder, sealed storage, away from moisture)
Product Datasheet
http://file.medchemexpress.com/batch_PDF/HY-100401A/Pactimibe-sulfate-DataSheet-MedChemExpress.pdf
Product MSDS
http://file.medchemexpress.com/batch_PDF/HY-100401A/Pactimibe-sulfate-SDS-MedChemExpress.pdf
Clinical Information
Phase 3
CAS Number
608510-47-0
Available Sizes
Curated Selection
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