Bempedoic acid (ETC-1002) 一种 ATP-柠檬酸裂解酶抑制剂

来源: MedChemExpress LLC   2019-12-31   访问量:588评论(0)

产品介绍:

Bempedoic acid (ETC-1002) 是一种 ATP-柠檬酸裂解酶 (ATP-citrate lyase;ACL) 抑制剂。Bempedoic acid (ETC-1002) 激活 AMPK

靶点:AMPK

体外作用:

Bempedoic acid (ETC-1002) activates AMP-activated protein kinase in a Ca2+/calmodulin-dependent kinase β-independent and liver kinase β 1-dependent manner, without detectable changes in adenylate energy charge. Bempedoic acid is shown to rapidly form a CoA thioester in liver, which directly inhibits ATP-citrate lyase[1]. In cells treated with Bempedoic acid (ETC-1002), increased levels of AMP-activated protein kinase (AMPK) phosphorylation coincide with reduced activity of MAP kinases and decreased production of proinflammatory cytokines and chemokines[2].

体内作用:

A marked and sustained increase in AMPK and ACC phosphorylation is found in rat livers following two weeks of treatment with Bempedoic acid (ETC-1002). Bempedoic acid is >100-fold more prevalent than the CoA thioester in rat liver and is associated with AMPK activation[1]. Bempedoic acid (ETC-1002) suppresses thioglycollate-induced homing of leukocytes into mouse peritoneal cavity. In a mouse model of diet-induced obesity, Bempedoic acid restores adipose AMPK activity, reduces JNK phosphorylation, and diminishes expression of macrophage-specific marker 4F/80[2].

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