全部分类
  • ETC-1002 (ESP-55016)
ETC-1002 (ESP-55016)的可视化放大

ETC-1002 (ESP-55016)

A prodrug form of ETC-1002-CoA

此产品仅用于科学研究,我们不为任何个人用途提供产品和服务

ETC-1002 (ESP-55016)的二维码
  • 库存: 现货
可选规格
  • 包装
    价格
    促销价
    数量
  • 5mg
    ¥600.00
    480.00
    - +
  • 10mg
    ¥875.00
    700.00
    - +
  • 50mg
    ¥2937.00
    2350.00
    - +
  • 100mg
    ¥4850.00
    3880.00
    - +
已选 0 0
金额: ¥0.00
首页 收藏
  • 货号: ajce51762
  • CAS: 738606-46-7
  • 别名: 贝派地酸,ETC-1002; ESP-55016
  • 分子式: C19H36O5
  • 分子量: 344.49
  • 纯度: >98%
  • 溶解度: DMSO : 100 mg/mL (290.28 mM)
  • 储存: Store at -20°C
  • 库存: 现货

Background

ETC-1002 is a prodrug form of ETC-1002-CoA.1 ETC-1002 is conjugated to coenzyme A (CoA) by very long-chain acyl-CoA synthetase-1 (ACSVL1) to form ETC-1002-CoA, which inhibits ATP citrate lyase (Ki = 2 μM) and activates AMP-activated protein kinase (AMPK). ETC-1002 suppresses total lipid synthesis in wild-type and AMPKβ1 knockout primary murine hepatocytes. In vivo, ETC-1002 (30 mg/kg) prevents increases in hepatic cholesterol and reduces the size of aortic atherosclerotic lesions induced by a high-fat high-cholesterol diet in Apoe-/-/Ampkβ1-/- (DKO) mice.


1.Pinkosky, S.L., Newton, R.S., Day, E.A., et al.Liver-specific ATP-citrate lyase inhibition by bempedoic acid decreases LDL-C and attenuates atherosclerosisNat. Commun.7:13457(2016)

Protocol

Cell experiment:

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].

Animal experiment:

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 Following nutritional staging and/or dosing, food is withdrawn 2 h prior to last the oral dose of ehicle control or Bempedoic acid[1].

参考文献:

[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.

没有评价数据

温馨提示 ×
商品已成功加入购物车!
购物车共 0 件商品
去购物车结算