1. Metabolic Enzyme/Protease PI3K/Akt/mTOR Epigenetics
  2. ATP Citrate Lyase AMPK
  3. Bempedoic acid

Bempedoic acid  (Synonyms: ETC-1002; ESP-55016)

目录号: HY-12357 含量: 98.99%
COA 产品使用指南

Bempedoic acid (ETC-1002) 是一种 ATP-柠檬酸裂解酶 (ATP-citrate lyase;ACL) 抑制剂。Bempedoic acid (ETC-1002) 激活 AMPK

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Bempedoic acid Chemical Structure

Bempedoic acid Chemical Structure

CAS No. : 738606-46-7

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3.  试用装只面向终端客户

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥610
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1 mg ¥250
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5 mg ¥550
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10 mg ¥800
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50 mg ¥2700
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100 mg ¥4500
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500 mg   询价  

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Other Forms of Bempedoic acid:

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Top Publications Citing Use of Products
  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Bempedoic acid (ETC-1002) is an ATP-citrate lyase (ACL) inhibitor[1]. Bempedoic acid (ETC-1002) activates AMPK[2].

IC50 & Target[1]

AMPK

 

体外研究
(In Vitro)

Bempedoic acid (ETC-1002) activates AMP-activated protein kinase in a Ca2+/calmodulin-dependent kinase β-independent and liver kinase β 1-dependent manner, without detectable changes in adenylate energy charge. Bempedoic acid is shown to rapidly form a CoA thioester in liver, which directly inhibits ATP-citrate lyase[1]. In cells treated with Bempedoic acid (ETC-1002), increased levels of AMP-activated protein kinase (AMPK) phosphorylation coincide with reduced activity of MAP kinases and decreased production of proinflammatory cytokines and chemokines[2].

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

体内研究
(In Vivo)

A marked and sustained increase in AMPK and ACC phosphorylation is found in rat livers following two weeks of treatment with Bempedoic acid (ETC-1002). Bempedoic acid is >100-fold more prevalent than the CoA thioester in rat liver and is associated with AMPK activation[1]. Bempedoic acid (ETC-1002) suppresses thioglycollate-induced homing of leukocytes into mouse peritoneal cavity. In a mouse model of diet-induced obesity, Bempedoic acid restores adipose AMPK activity, reduces JNK phosphorylation, and diminishes expression of macrophage-specific marker 4F/80[2].

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

Clinical Trial
分子量

344.49

Formula

C19H36O5

CAS 号
性状

固体

颜色

White to light yellow

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 (290.28 mM; 超声助溶; 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 2.9028 mL 14.5142 mL 29.0284 mL
5 mM 0.5806 mL 2.9028 mL 5.8057 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

In Vivo:

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂: 5% DMSO    40% PEG300    5% Tween-80    50% Saline

    Solubility: ≥ 2.87 mg/mL (8.33 mM); 澄清溶液

  • 方案 二

    请依序添加每种溶剂: 5% DMSO    95% (20% SBE-β-CD in Saline)

    Solubility: 2.87 mg/mL (8.33 mM); 悬浊液; 超声助溶

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
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 98.99%

参考文献
Cell Assay
[1]

Glucose production is measured in primary rat hepatocyte cultures. Cells are cultured in glucose- and phenol red-free DMEM, containing 10 mM lactate, 1 mM pyruvate, and nonessential amino acids. Cells are incubated with various concentrations of Bempedoic acid (0.1 to 100 μM)[1].

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

Animal Administration
[1]

Rats: Prior to single-dose Bempedoic acid administration, Male Wistar Han rats are fasted for 48 h and refed a high-carbohydrate diet for an additional 48 h. For two-week assessment, rats are maintained on standard chow diet and dosed by oral gavage with Bempedoic acid at 30 mg/kg/day for two weeks in the morning. Following nutritional staging and/or dosing, food is withdrawn 2 h prior to last the oral dose of ehicle control or Bempedoic acid[1].

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

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 2.9028 mL 14.5142 mL 29.0284 mL 72.5710 mL
5 mM 0.5806 mL 2.9028 mL 5.8057 mL 14.5142 mL
10 mM 0.2903 mL 1.4514 mL 2.9028 mL 7.2571 mL
15 mM 0.1935 mL 0.9676 mL 1.9352 mL 4.8381 mL
20 mM 0.1451 mL 0.7257 mL 1.4514 mL 3.6286 mL
25 mM 0.1161 mL 0.5806 mL 1.1611 mL 2.9028 mL
30 mM 0.0968 mL 0.4838 mL 0.9676 mL 2.4190 mL
40 mM 0.0726 mL 0.3629 mL 0.7257 mL 1.8143 mL
50 mM 0.0581 mL 0.2903 mL 0.5806 mL 1.4514 mL
60 mM 0.0484 mL 0.2419 mL 0.4838 mL 1.2095 mL
80 mM 0.0363 mL 0.1814 mL 0.3629 mL 0.9071 mL
100 mM 0.0290 mL 0.1451 mL 0.2903 mL 0.7257 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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HY-12357
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