ETC-1002 (ESP-55016) (Synonyms: Bempedoic Acid, ESP-55016) |
Catalog No.GC33760 |
ETC-1002(ESP-55016)(ETC-1002)는 ATP-시트레이트 리아제(ACL) 억제제입니다.
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Cas No.: 738606-46-7
Sample solution is provided at 25 µL, 10mM.
ETC-1002 is an activator of hepatic AMP-activated protein kinase (AMPK).
ETC-1002 free acid 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. ETC-1002 is shown to rapidly form a CoA thioester in liver, which directly inhibits ATP-citrate lyase[1]. In cells treated with 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].
A marked and sustained increase in AMPK and ACC phosphorylation is found in rat livers following two weeks of treatment with ETC-1002. ETC-1002 free acid is >100-fold more prevalent than the CoA thioester in rat liver and is associated with AMPK activation[1]. ETC-1002 suppresses thioglycollate-induced homing of leukocytes into mouse peritoneal cavity. 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[2].
[1]. Pinkosky SL, et al. AMP-activated protein kinase and ATP-citrate lyase are two distinct molecular targets for ETC-1002, a novel small molecule regulator of lipid and carbohydrate metabolism. J Lipid Res. 2013 Jan;54(1):134-51. [2]. Filippov S, et al. ETC-1002 regulates immune response, leukocyte homing, and adipose tissue inflammation via LKB1-dependent activation of macrophage AMPK. J Lipid Res. 2013 Aug;54(8):2095-108.
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