2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
生物活性
Description
In Vivo
In Vitro
化合物的使用
Kinase Assay
Cell Assay
Animal Administration
参考文献
ETC-1002(ESP-55016) is a novel, first-in-class, orally available, once-daily LDL-C lowering small molecule; activator of hepatic AMP-activated protein kinase (AMPK); also has potent inhibitory activity against hepatic ATP-citrate lyase(IC50=29 uM).
in vitro: ETC-1002 free acid activates AMP-activated protein kinase in a Ca(2+)/calmodulin-dependent kinase β-independent and liver kinase β 1-dependent manner, without detectable changes in adenylate energy charge. Furthermore, ETC-1002 is shown to rapidly form a CoA thioester in liver, which directly inhibits ATP-citrate lyas. In cells treated with ETC-1002, increased levels of AMP-activated protein kinase (AMPK) phosphorylation coincided with reduced activity of MAP kinases and decreased production of proinflammatory cytokines and chemokines .
in vivo: Activation of hepatic AMPK with ETC-1002 treatment from the two-week Wistar rat study was not associated with altered hepatic AEC. however, ETC-1002 treatment coincided with a 70% reduction in hepatic TG, while low basal levels of CE and FC remained insensitive to treatment. Importantly, reductions in liver TG content was accompanied by 51% increase in plasma β-HBA, indicating enhanced liver fatty acid β-oxidation . ETC-1002 suppressed thioglycollate-induced homing of leukocytes into mouse peritoneal cavity. Similarly, in a mouse model of diet-induced obesity, ETC-1002 restored adipose AMPK activity, reduced JNK phosphorylation, and diminished expression of macrophage-specific marker 4F/80.
For the detailed information of Bempedoic Acid(ETC-1002;ESP-55016), the solubility of Bempedoic Acid(ETC-1002;ESP-55016) in water, the solubility of Bempedoic Acid(ETC-1002;ESP-55016) in DMSO, the solubility of Bempedoic Acid(ETC-1002;ESP-55016) in PBS buffer, the animal experiment (test) of Bempedoic Acid(ETC-1002;ESP-55016), the cell expriment (test) of Bempedoic Acid(ETC-1002;ESP-55016), the in vivo, in vitro and clinical trial test of Bempedoic Acid(ETC-1002;ESP-55016), the EC50, IC50,and affinity,of Bempedoic Acid(ETC-1002;ESP-55016), For the detailed information of Bempedoic Acid(ETC-1002;ESP-55016), the solubility of Bempedoic Acid(ETC-1002;ESP-55016) in water, the solubility of Bempedoic Acid(ETC-1002;ESP-55016) in DMSO, the solubility of Bempedoic Acid(ETC-1002;ESP-55016) in PBS buffer, the animal experiment (test) of Bempedoic Acid(ETC-1002;ESP-55016), the cell expriment (test) of Bempedoic Acid(ETC-1002;ESP-55016), the in vivo, in vitro and clinical trial test of Bempedoic Acid(ETC-1002;ESP-55016), the EC50, IC50,and affinity,of Bempedoic Acid(ETC-1002;ESP-55016), Please contact DC Chemicals.
