化合物ETC1002 T3625

Product Introduction
Bioactivity


英文名: Bempedoic acid

描述: Bempedoic acid (ETC1002) 是一种 ATP-柠檬酸裂解酶抑制剂，可激活AMPK。它是脂质和碳水化合物代谢的调节剂。

细胞实验: Primary rat hepatocytes and differentiated human MDMs are treated with indicated concentrations of ETC-1002 for 12 h. Working solutions of ETC-1002 are prepared in serum-free RPMI 1640 containing 12 mM HEPES, 10,000 U/ml penicillin, and 100 μg/ml streptomycin. (Only for Reference)

激酶实验: 7.5× compounds are added to a 96-well PolyPlate containing 60 μL of Buffer per well with substrates CoA (200 μM), ATP (400 μM), and [14C]citrate. Reaction is started with 4 μL (300 ng/well) ACL, and the plate is incubated at 37°C for 3 h. Th

体外活性: ETC-1002是一种处于非活化状态的前体药物,在体内通过内源性肝脏ACS活性转化为ACL抑制剂（活化状态,ECT-1002-CoA）.ETC-1002抑制硫胶质诱导的白血球向小鼠腹膜腔的迁移.ETC-1002可恢复饮食诱导型肥胖症的小鼠模型中脂肪AMPK活性,降低JNK磷酸化,减少巨噬细胞特异marker 4F/80的表达.

体内活性: TC-1002作用机制主要是靶向两种肝酶: 腺苷三磷酸-枸橡酸裂解酶（ACL）和腺苷酸活化蛋白激酶（AMPK）,抑制甾醇和脂肪酸合成并促进线粒体长链脂肪酸的氧化。ETC-1002提高AMPK磷酸化水平,降低MAPKs的活性以及减少促炎细胞因子和趋化因子的产生。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 63 mg/mL (182.9 mM)


关键字: Bempedoic acid | ESP 55016 | ATP Citrate Lyase | inhibit | Inhibitor | ESP55016 | AMP-activated protein kinase | ACLY | AMPK

相关产品: Hydroxycitric acid tripotassium hydrate | Forrestiacids K | BMS-303141 | SB 204990 | Forrestiacids J | MEDICA16 | NDI-091143 | 2-Furoic acid | (-)-Hydroxycitric acid lactone | (-)-Hydroxycitric acid

相关库: Drug Repurposing Compound Library | FDA-Approved Kinase Inhibitor Library | FDA-Approved & Pharmacopeia Drug Library | Anti-Cancer Drug Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Kinase Inhibitor Library | Anti-Cancer Approved Drug Library | EMA Approved Drug Library | Orally Active Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途