FSL0392
- Structure
- InChI=1S/C19H20F3NO2.ClH/c1-14(12-15-6-5-9-17(13-15)19(20,21)22)23-10-11-25-18(24)16-7-3-2-4-8-16;/h2-9,13-14,23H,10-12H2,1H3;1H
- InChIKey=NLOALSPYZIIXEO-UHFFFAOYSA-N
- Synonyms
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- 23602-78-0
- Benfluorex hydrochloride
- Origin
- Chemically synthesized
- Biological activities
- Activate the nuclear receptor transcription factor HNF4a
- Therapeutic
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Anorectic
Antihyperglycemic
Hypolipidemic
- Target
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HNF4a
- Assay information
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Used to treat hyperlipidemia and type II diabetes, induction of the reduction in cofactor availability (acetyl-CoA, NADH, and ATP) as the result of the inhibition of β-oxidation
Inhibition of hepatic lipogenesis and triglyceride and sterol synthesis
Hit compoudns in the human insulin promotor lipotoxicity reversal screen using T6PNE cells (EC50 = 24.4 μM)
Interaction with and activation of HNF4α directly shown by DARTS experiment
- References
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Lee SH, Athavankar S, Cohen T, Piran R, Kiselyuk A, Levine F
Identification of alverine and benfluorex as HNF4α activators.
ACS Chem Biol, 8(8): 1730-1736 (2013) 23675775 doi: 10.1021/cb4000986
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Kohl C, Ravel D, Girard J, Pégorier JP
Effects of benfluorex on fatty acid and glucose metabolism in isolated rat hepatocytes: from metabolic fluxes to gene expression.
Diabetes, 51(8): 2363-2368 (2002) 12145146
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Ravel D, Laudignon N
Research prospects with benfluorex.
J Diabetes Complications, 10(5): 246-254 (1996) 8887012
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Jacques Duhault
(1980). Treatment of carbohydrate metabolism disorders. US4237165.