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

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.

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P053 Chemical Structure

P053 Chemical Structure

CAS No. : 2748196-63-4

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

P053 Related Antibodies

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ACAT1 ACAT2 MGAT2 ACAT

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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].

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

P053 Related Antibodies
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].

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

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
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (282.27 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8227 mL 14.1135 mL 28.2271 mL
5 mM 0.5645 mL 2.8227 mL 5.6454 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8227 mL 14.1135 mL 28.2271 mL 70.5676 mL
5 mM 0.5645 mL 2.8227 mL 5.6454 mL 14.1135 mL
10 mM 0.2823 mL 1.4114 mL 2.8227 mL 7.0568 mL
15 mM 0.1882 mL 0.9409 mL 1.8818 mL 4.7045 mL
20 mM 0.1411 mL 0.7057 mL 1.4114 mL 3.5284 mL
25 mM 0.1129 mL 0.5645 mL 1.1291 mL 2.8227 mL
30 mM 0.0941 mL 0.4705 mL 0.9409 mL 2.3523 mL
40 mM 0.0706 mL 0.3528 mL 0.7057 mL 1.7642 mL
50 mM 0.0565 mL 0.2823 mL 0.5645 mL 1.4114 mL
60 mM 0.0470 mL 0.2352 mL 0.4705 mL 1.1761 mL
80 mM 0.0353 mL 0.1764 mL 0.3528 mL 0.8821 mL
100 mM 0.0282 mL 0.1411 mL 0.2823 mL 0.7057 mL
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P053 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

P0532748196-63-4P 053P-053AcyltransferaseDiacylglycerol acyltransferaseDiglyceride acyltransferaseacyl-CoA:cholesterol acyltransferasemono- acylglycerol acyltransferaseceramidesynthaseCerS1endogenousmitochondrialfattyacidoxidationmuscleadiposityInhibitorinhibitorinhibit

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