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

P053 

目录号: HY-126015
产品使用指南

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 为 0.5 μM。P053 作为肌肉线粒体脂肪酸氧化的内源性抑制剂。全身肥胖调节剂。

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P053 Chemical Structure

P053 Chemical Structure

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     可免费申领三个不同产品的试用装。

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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[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]

体外研究
(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].

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

体内研究
(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].

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.
分子量

354.27

Formula

C₁₈H₂₁Cl₂NO₂

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2

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目录号:
HY-126015
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