产品
编 号:F741752
分子式:C18H21Cl2NO2
分子量:354.27
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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生物活性:
P053 is a potent, non-competitive and selective ceramide synthase 1 (CerS1) inhibitor wirh an IC50 of 0.5?μM. P053 acts as an endogenous inhibitor of mitochondrial fatty acid oxidation in muscle. Whole-body adiposity regulator.

体内研究:
P053 (5?mg/kg; administered daily by oral gavage; 7 days, in male C57BL6/J mice ) reduces C18 ceramide levels in skeletal muscle (SkM) .Daily P053 administration to mice fed a high-fat diet (HFD) increases fatty acid oxidation in skeletal muscle and impedes increases in muscle triglycerides and adiposity, but does not protect against HFD-induced insulin resistance.Animal Model:Male C57BL6/J mice
Dosage:5?mg/kg
Administration:Oral gavage; daily
Result:Reduced C18 ceramide levels in SkM by 31%, whereas 1?mg/kg/day had no effect.

体外研究:
P053 is the first isoform-specific ceramide synthase inhibitor. P053 inhibits CerS1 with nanomolar potency. P053 inhibits different human (h) or murine (m) CerS isoforms hCerS1, mCerS1, hCerS2, mCerS2, hCerS4, mCerS5, and hCerS6 with IC50s of 0.54±0.06, 0.46±0.08, 28.6±0.15, 18.5±0.12, 17.2±0.09, 7.2±0.10, and 11.4±0.17 μM, respectively.
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