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Chemical Structure : F12511
Catalog No.: PC-49562Not For Human Use, Lab Use Only.
Eflucimibe (F 12511) is a highly potent, selective inhibitor of acyl-CoA: cholesterol acyltransferase ( ACAT/SOAT) with IC50 of 3, 7, and 71 nM in whole cell assays using HepG2, CaCo-2 and THP-1 cell lines, respectively.
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Eflucimibe (F 12511) is a highly potent, selective inhibitor of acyl-CoA: cholesterol acyltransferase ( ACAT/SOAT) with IC50 of 3, 7, and 71 nM in whole cell assays using HepG2, CaCo-2 and THP-1 cell lines, respectively.
F 12511 potently inhibits ACAT activity in microsomal preparations from various animal species as well as of cholesterol esterification in relevant human cell lines in culture.
F 12511 inhibits ACAT activity in microsomal preparations with EC values ranged from 41 nM for hypercholesterolemic rabbit intestine to 223 nM for normocholesterolemic hamster liver.
Orally administered F 12511 displayed high potency and efficacy as an antihypercholesterolemic compound in different cholesterol-fed animals (rat, guinea-pig, rabbit), reduced plasma cholesterol levels in guinea-pigs with ED30 of 0.008 mg/kg.
F 12511 lowered plasma cholesterol levels in New Zealand rabbits fed a cholesterol-free casein-rich diet.
| M.Wt | 469.728 | |
| Formula | C29H43NO2S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Junquero D, et al. Biochem Pharmacol. 2001 Jan 1;61(1):97-108.
2. Junquero D, et al. Atherosclerosis. 2001 Mar;155(1):131-42.
3. Zamorano-León JJ, et al. J Cardiovasc Pharmacol. 2006 Sep;48(3):128-34.
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