1. Metabolic Enzyme/Protease
  2. Acyltransferase
  3. P053

P053 

Cat. No.: HY-126015
Handling Instructions

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.

For research use only. We do not sell to patients.

P053 Chemical Structure

P053 Chemical Structure

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Description

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[1].

IC50 & Target

IC50: 0.54±0.06 μM (hCerS1), 0.46±0.08 μM (mCerS1), 28.6±0.15 μM (hCerS2), 18.5±0.12 μM (mCerS2), 17.2±0.09 μM (hCerS4), 7.2±0.10 μM (mCerS5), 11.4±0.17 μM (hCerS6)[1]

In Vitro

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[1].

In Vivo

P053 (5 mg/kg; administered daily by oral gavage; 7 days, in male C57BL6/J mice ) reduces 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, but does 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.
Molecular Weight

354.27

Formula

C₁₈H₂₁Cl₂NO₂

SMILES

OC[[email protected]@](C)(N)CCC1=CC=C(OCC2=CC=C(Cl)C(Cl)=C2)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

P053P 053P-053AcyltransferaseDiacylglycerol acyltransferaseDiglyceride acyltransferaseacyl-CoA:cholesterol acyltransferasemono- acylglycerol acyltransferaseceramidesynthaseCerS1endogenousmitochondrialfattyacidoxidationmuscleadiposityInhibitorinhibitorinhibit

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P053
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