P053 - 10mM in DMSO , CAS No.2748196-63-4

CAS: 2748196-63-4 Cat. No.: P654495 Molecular Weight: 354.27

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

P053 is a potent, non-competitive and selective ceramide synthase 1 ( CerS1 ) inhibitor wirh an IC 50 of 0.5 μM. P053 acts as an endogenous inhibitor of mitochondrial fatty acid oxidation in muscle. Whole-body adiposity regulator

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 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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) . 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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.

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)

Specifications

Specifications & Purity

10mM in DMSO

Biochemical and Physiological Mechanisms

P053 is a potent, non-competitive and selective ceramide synthase 1 ( CerS1 ) inhibitor wirh an IC 50 of 0.5u2009μM. P053 acts as an endogenous inhibitor of mitochondrial fatty acid oxidation in muscle. Whole-body adiposity regulator.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Action Type

INHIBITOR

Names and Identifiers

• Molecular Weight: 354.27