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

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

CAS No. : 2748196-63-4

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     可免费申领三个不同产品的试用装。

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥5500
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1 mg ¥2000
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5 mg ¥5000
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10 mg ¥8500
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100 mg   询价  

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Customer Review

查看 Acyltransferase 亚型特异性产品:

  • 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

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 100 mg/mL (282.27 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 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
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: ≥97.0%

参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 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
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.

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产品名称:
P053
目录号:
HY-126015
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