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- 详细信息
- 文献和实验
- 技术资料
- 保存条件：
Powder:-20℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 保质期：
Powder:-20℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 英文名：
Bempedoic Acid
- 库存：
现询
- 供应商：
北京索莱宝科技有限公司
- CAS号：
738606-46-7
- 规格：
100mg/50mg/1mg/10mg/5mg
| 规格： | 100mg | 产品价格： | ￥4490.0 |
|---|---|---|---|
| 规格： | 50mg | 产品价格： | ￥2690.0 |
| 规格： | 1mg | 产品价格： | ￥240.0 |
| 规格： | 10mg | 产品价格： | ￥790.0 |
| 规格： | 5mg | 产品价格： | ￥540.0 |
| 基本信息 | |
| CAS | No.738606-46-7 |
| 中文名称 | 贝派地酸 |
| 英文名称 | Bempedoic Acid |
| 别名 | ESP-55016;ETC1002 |
| 分子式 | C19H36O5 |
| 分子量 | 344.49 |
| 溶解性 | Soluble in DMSO |
| 纯度 | ≥98% |
| 外观(性状) | White to yellow Solid |
| 储存条件 | Powder:-20℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| SMILES | CC(C)(CCCCCC(CCCCCC(C)(C)C(=O)O)O)C(=O)O |
| 靶点 | ATPCitrate Lyase (ACL)，AMPK |
| 通路 | PI3K/Akt/mTOR;Epigenetics |
| 背景说明 | Bempedoic Acid是一种 ATP-柠檬酸裂解酶 (ATP-citrate lyase (ACL)) 抑制剂,可以激活 AMPK。 |
| 生物活性 | Bempedoic acid (ETC-1002) is an ATP-citrate lyase (ACL) inhibitor[1]. Bempedoic acid (ETC-1002) activates AMPK[2]. |
| IC50 | AMPK |
| 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]. |
| 细胞实验 | 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]. |
| 细胞实验 | 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]. |
| 动物实验 | 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]. |
| 数据来源文献 | [1]. Pinkosky SL， et al. AMP-activated protein kinase and ATP-citrate lyase are two distinct molecular targets for ETC-1002， a novel small molecule regulator of lipid and carbohydrate metabolism. J Lipid Res. 2013 Jan;54(1):134-51. [2]. Filippov S， et al. ETC-1002 regulates immune response， leukocyte homing， and adipose tissue inflammation via LKB1-dependent activation of macrophage AMPK. J Lipid Res. 2013 Aug;54(8):2095-108. |
| 单位 | 瓶 |
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