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Pactimibe sulfate

Cat. No. M30357

All AbMole products are for research use only, cannot be used for human consumption.

Pactimibe sulfate Structure
Synonym:

CS-505

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Quality Control & Documentation
Biological Activity

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. 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.

Chemical Information
Molecular Weight 465.65
Formula C25H40N2O3.1/2H2O4S
CAS Number 608510-47-0
Form Solid
Solubility (25°C) DMSO 100 mg/mL (ultrasonic)
Storage 4°C, dry, sealed
References

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

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

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

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

[5] Naoki Terasaka, et al. Atherosclerosis. ACAT inhibitor pactimibe sulfate (CS-505) reduces and stabilizes atherosclerotic lesions by cholesterol-lowering and direct effects in apolipoprotein E-deficient mice

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Keywords: Pactimibe sulfate, CS-505 supplier, Transferase, inhibitors, activators

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