ETC-1002 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。

ETC-1002, also known as ESP-55016 and 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. Bempedoic acid is absorbed rapidly in the small intestine and enters the liver through cell surface receptors different from those transporters that selectively take up statins. Bempedoic acid is a regulator of lipid and carbohydrate metabolism.

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.

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。

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

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)

738606-46-7

C19H36O5

344.49

ESP-55016;ETC-1002;ETC 1002;ETC1002

H2O:<1 mgml
DMSO:63 mg/mL (182.9 mM)
Ethanol:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years