P053 是一种有效的，非竞争性和选择性的神经酰胺合酶1 (CerS1) 抑制剂（IC50= 0.5 μM）。P053 作为肌肉线粒体脂肪酸氧化的内源性抑制剂和全身肥胖调节剂。

P053 is a potent, non-competitive and selective ceramide synthase 1 (CerS1) inhibitor with an IC50 of 0.5 μM. P053 is an endogenous inhibitor of mitochondrial fatty acid oxidation in muscle and regulator of whole-body adiposity[1].

P053 is the first isoform-specific ceramide synthase inhibitor with nanomolar potency. P053 inhibits different human (h) or murine (m) CerS isoforms hCerS1, mCerS1, hCerS2, mCerS2, hCerS4, mCerS5, and hCerS6 with IC 50 s 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 [1].

P053 (5 mg/kg; administered daily by oral gavage; 7 days, in male C57BL6/J mice ) lowers C18 ceramide levels in skeletal muscle (SkM) [1]. 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 while not protect against HFD-induced insulin resistance [1]. Animal Model: Male C57BL6/J mice [1] 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.

2748196-63-4

C18H21Cl2NO2

354.27

P053

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years