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Pactimibe

Cat. No. M28998

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Pactimibe Structure
Synonym:

CS-505 free base

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Quality Control & Documentation
Biological Activity

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. 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.

Chemical Information
Molecular Weight 416.6
Formula C25H40N2O3
CAS Number 189198-30-9
Form Solid
Solubility (25°C) DMSO 120 mg/mL (ultrasonic)
Storage 4°C, dry, sealed
References

[1] M Kotsuma, et al. Int J Clin Pharmacol Ther. Effect of CYP2D6 polymorphism on pharmacokinetics of a novel ACAT inhibitor, pactimibe and its unique metabolite, R-125528

[2] Masakatsu Kotsuma, et al. Drug Metab Dispos. Effects of ketoconazole and quinidine on pharmacokinetics of pactimibe and its plasma metabolite, R-125528, in humans

[3] Ken Kitayama, et al. Eur J Pharmacol. Multiple mechanisms of hypocholesterolemic action of pactimibe, a novel acyl-coenzyme A:cholesterol acyltransferase inhibitor

[4] Ken Kitayama, et al. Eur J Pharmacol. Importance of acyl-coenzyme A:cholesterol acyltransferase 1/2 dual inhibition for anti-atherosclerotic potency of pactimibe

[5] Ken Kitayama, et al. Eur J Pharmacol. Pactimibe stabilizes atherosclerotic plaque through macrophage acyl-CoA:cholesterol acyltransferase inhibition in WHHL rabbits

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Keywords: Pactimibe, CS-505 free base supplier, Transferase, inhibitors, activators

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