|ETC-1002 (ESP-55016) Catalog No.GC33760|
Sample solution is provided at 25 µL, 10mM.
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Glucose production is measured in primary rat hepatocyte cultures. Cells are cultured in glucose- and phenol red-free DMEM, containing 10 mM lactate, 1 mM pyruvate, and nonessential amino acids. Cells are incubated with various concentrations of Bempedoic acid (0.1 to 100 μM).
Rats: Prior to single-dose Bempedoic acid administration, Male Wistar Han rats are fasted for 48 h and refed a high-carbohydrate diet for an additional 48 h. For two-week assessment, rats are maintained on standard chow diet and dosed by oral gavage with Bempedoic acid at 30 mg/kg/day for two weeks in the morning. Following nutritional staging and/or dosing, food is withdrawn 2 h prior to last the oral dose of ehicle control or Bempedoic acid.
. 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.
|Cas No.||738606-46-7||SDF||Download SDF|
|Chemical Name||8-hydroxy-2,2,14,14-tetramethylpentadecanedioic acid|
|Solubility||DMSO : 100 mg/mL (290.28 mM; Need ultrasonic)||Storage||Store at -20°C|
|General tips||For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.|
|Shipping Condition||Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
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. 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.
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. 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.
. 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. . 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.