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  • ETC-1002
    • Bempedoic Acid;ESP-55016;SGI-7079
    货号: abs816180
    CAS号: 738606-46-7
    分子式: C19H36O5
    分子量: 455.53
    产品说明书
    分享:
    货号-规格 货期 价格 数量
    abs816180-2mg 1-2周 ¥667.00
    - +
    abs816180-5mg 1-2周 ¥1067.00
    - +
    abs816180-10mg 1-2周 ¥1637.00
    - +
    abs816180-20mg 1-2周 ¥2756.00
    - +
    大包装询价
    产品描述
    描述

    ETC-1002,also known as Bempedoic acid, is an orally available, once-daily LDL-C lowering small molecule designed to lower elevated levels of LDL-C and to avoid side effects associated with existing LDL-C lowering therapies.ETC-1002 is an activator of hepatic AMP-activated protein kinase (AMPK). It has potent inhibitory activity against hepatic ATP-citrate lyase(IC50=29 uM).

    纯度
    98%
    储存/保存方法
    store at -20℃ for one year(Powder);
    in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.
    基本信息
    别名
    Bempedoic Acid;ESP-55016;SGI-7079
    可溶性/溶解性
    DMSO : 63 mg/mL (182.9 mM)
    生物活性
    靶点
    AMPK
    In vitro(体外研究)
    ETC-1002 is a new investigational low density lipoprotein cholesterol (LDL-C)-lowering agent which is a dicarboxylic acid derivative with a novel mechanism of action targeting two hepatic enzymes--adenosine triphosphate-citrate lyase (ACL) and adenosine monophosphate-activated protein kinase (AMPK), inhibiting sterol and fatty acid synthesis and promoting mitochondrial long-chain fatty acid oxidation. It increases levels of AMP-activated protein kinase (AMPK) phosphorylation, reduces activity of MAP kinases and decreases production of proinflammatory cytokines and chemokines. These effects on soluble mediators of inflammation can be significantly abrogated by LKB1 siRNAs, indicating that ETC-1002 activates AMPK and exerts its anti-inflammatory effects via an LKB1-dependent mechanism.
    In vivo(体内研究)
    ETC-1002 suppresses thioglycollate-induced homing of leukocytes into mouse peritoneal cavity. Similarly, in a mouse model of diet-induced obesity, ETC-1002 restores adipose AMPK activity, reduces JNK phosphorylation, and diminishes expression of macrophage-specific marker 4F/80. ETC-1002 is an inactive prodrug and converted to an active ACL inhibitor(ECT-1002-CoA) by endogenous liver ACS activity in vivo.
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