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Lifibrol

Catalog No. T27832   CAS 96609-16-4
Synonyms: U 83860, K-12148, K-12.148, U-83860, K12148

Lifibrol (U-83860) is an inhibitor of cholesterol synthesis.Lifibrol has anticholesterol and hypolipidemic properties and promotes the conversion of LDL Apo B-100 in patients with hypercholesterolemia and mixed hyperlipidemia.

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Lifibrol Chemical Structure
Lifibrol, CAS 96609-16-4
Pack Size Availability Price/USD Quantity
1 mg In stock $ 146.00
5 mg In stock $ 350.00
10 mg In stock $ 530.00
25 mg In stock $ 859.00
50 mg In stock $ 1,180.00
100 mg In stock $ 1,590.00
500 mg In stock $ 3,190.00
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Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Lifibrol (U-83860) is an inhibitor of cholesterol synthesis.Lifibrol has anticholesterol and hypolipidemic properties and promotes the conversion of LDL Apo B-100 in patients with hypercholesterolemia and mixed hyperlipidemia.
In vivo Resident peritoneal macrophages isolated from rats pretreated with Lifibrol (50 mg/kg/7 days; mixed into the feed) showed a decreased capacity to synthesize cholesteryl esters from labeled precursors ([1-14C]oleate and [4-14C]cholesterol). Modification of lipid metabolism in atherosclerotic aortae from swine and Watanabe heritable hyperlipidemic (WHHL) rabbits was also observed when the tissues were incubated in vitro in the presence of exogenous Lifibrol.[5]
Concentrations of lifibrol of up to 50 micrograms/mL in the incubations selectively reduced the formation of cholesteryl esters from [1-14C]acetate by 60-75%, whereas higher concentrations (100 micrograms/mL) resulted in a generalized inhibition of lipid biosynthesis of about 50% and of cholesteryl ester formation by up to 90%. The ability of lifibrol to directly affect these targets (i.e. macrophages and arterial tissue) has implications that extend beyond its confirmed plasma cholesterol-lowering activity.[5]
Synonyms U 83860, K-12148, K-12.148, U-83860, K12148
Molecular Weight 342.43
Formula C21H26O4
CAS No. 96609-16-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (146.02 mM)

TargetMolReferences and Literature

1. Locker PK, et al. Lifibrol: a novel lipid-lowering drug for the therapy of hypercholesterolemia. Lifibrol Study Group. Clin Pharmacol Ther. 1995;57(1):73-88. 2. Winkler K, et al. Lifibrol enhances the low density lipoprotein apolipoprotein B-100 turnover in patients with hypercholesterolemia and mixed hyperlipidemia. Atherosclerosis. 1999;144(1):167-175. 3. Scharnagl H, et al. The effects of lifibrol (K12.148) on the cholesterol metabolism of cultured cells: evidence for sterol independent stimulation of the LDL receptor pathway. Atherosclerosis. 2000;153(1):69-80. 4. Sun EL, et al. Biotransformation of lifibrol (U-83860) to mixed glyceride metabolites by rat and human hepatocytes in primary culture. Drug Metab Dispos. 1996;24(2):221-231. 5. Bell FP. Effect of the lipid-lowering drug lifibrol on lipid metabolism in rat macrophages and in atherosclerotic arteries from swine and WHHL rabbits, in vitro. Implications in atherogenesis. Biochem Pharmacol. 1993;46(8):1475-1480.

Related compound libraries

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Keywords

Lifibrol 96609-16-4 Metabolism Lipid U 83860 K 12148 K-12148 U83860 K-12.148 U-83860 K12148 inhibitor inhibit

 

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