中文名：ETC-1002
英文名：ETC-1002
纯度：Moligand™，≥99%
货号：E413887
Cas号：738606-46-7
存储温度：-20°C储存
运输条件：超低温运输
产品介绍：
Information
ETC-1002 ETC-1002 (Bempedoic acid, ESP-55016),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).
Targets
AMPK
In vitro
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
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.
Cell Research(from reference)
Cell lines：Primary rat hepatocytes and differentiated human monocyte-derived macrophages
Concentrations：30 μM or 100 μM
Incubation Time：12 h
Application
Bempedoic Acid is used for the treatment of dyslipidemia and other cardio-metabolic risk factors . It inhibits ATP citrate lyase (ACL), which an enzyme involved in fatty acid and cholesterol synthesis.
查看阿拉丁官网此产品相关对应页面：https://www.aladdin-e.com/zh_cn/E413887.html
关键字： acido bempedoico ; CHEBI:44212 ; DB11936 ; (2R,3R)-rel-2,3-Dihydroxysuccinic acid
上海阿拉丁生化科技股份有限公司是A股上市公司（（股票代码：688179），专注于科研试剂的研发、生产和销售，已陆续建立多个工厂和研发中心。作为领军企业，阿拉丁始终坚持质量第一，连续13年被评为“最受欢迎试剂品牌”。
阿拉丁目前常备库存试剂产品品种超过7万种，SKU总数超过46万，产品线涵盖了化学试剂、生化试剂、药靶配体、蛋白质和抗体等多个领域，是国内少数化学试剂到生物试剂全面发展的国产试剂品牌，产品同步发布在我们国内外电商平台。