中文名：ETC-1002
英文名：ETC-1002
純度：Moligand?，≥99%
貨號(hào)：E413887
Cas號(hào)：738606-46-7
存儲(chǔ)溫度：-20°C儲(chǔ)存
運(yùn)輸條件：超低溫運(yùn)輸
產(chǎn)品介紹：
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.
查看阿拉丁官網(wǎng)此產(chǎn)品相關(guān)對(duì)應(yīng)頁面：https://www.aladdin-e.com/zh_cn/E413887.html
關(guān)鍵字： 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（（股票代碼：688179），專注于科研試劑的研發(fā)、生產(chǎn)和銷售，已陸續(xù)建立多個(gè)工廠和研發(fā)中心。作為領(lǐng)軍企業(yè)，阿拉丁始終堅(jiān)持質(zhì)量第一，連續(xù)13年被評(píng)為“最受歡迎試劑品牌”。
阿拉丁目前常備庫(kù)存試劑產(chǎn)品品種超過7萬種，SKU總數(shù)超過46萬，產(chǎn)品線涵蓋了化學(xué)試劑、生化試劑、藥靶配體、蛋白質(zhì)和抗體等多個(gè)領(lǐng)域，是國(guó)內(nèi)少數(shù)化學(xué)試劑到生物試劑全面發(fā)展的國(guó)產(chǎn)試劑品牌，產(chǎn)品同步發(fā)布在我們國(guó)內(nèi)外電商平臺(tái)。