Pactimibe

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].

Product Specifications

CAS Number

[189198-30-9]

Product Name Alternative

CS-505 (free base)

UNSPSC

12352005

Target

Acyltransferase

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

Neuroscience-Neuromodulation

Field of Research

Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/pactimibe.html

Purity

99.98

Solubility

DMSO : 200 mg/mL (ultrasonic)

Smiles

O=C(O)CC1=C(C)C2=C(N(CCCCCCCC)CC2)C(NC(C(C)(C)C)=O)=C1C

Molecular Formula

C25H40N2O3

Molecular Weight

416.60

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)

Scientific Category

Reference compound1

Clinical Information

Phase 3

Isoform

ACAT; ACAT1; ACAT2

Available Sizes

Curated Selection

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