Catalog No.S7953 Synonyms: Bempedoic acid, ESP-55016
Molecular Weight(MW): 344.49
ETC-1002,also known as 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.ETC-1002 is an activator of hepatic AMP-activated protein kinase (AMPK). It has potent inhibitory activity against hepatic ATP-citrate lyase(IC50=29 uM).
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|Description||ETC-1002,also known as 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.ETC-1002 is an activator of hepatic AMP-activated protein kinase (AMPK). It has potent inhibitory activity against hepatic ATP-citrate lyase(IC50=29 uM).|
ETC-1002 is a new investigational low density lipoprotein cholesterol (LDL-C)-lowering agent which is a dicarboxylic acid derivative with a novel mechanism of action targeting two hepatic enzymes--adenosine triphosphate-citrate lyase (ACL) and adenosine monophosphate-activated protein kinase (AMPK), inhibiting sterol and fatty acid synthesis and promoting mitochondrial long-chain fatty acid oxidation. It increases levels of AMP-activated protein kinase (AMPK) phosphorylation, reduces activity of MAP kinases and decreases production of proinflammatory cytokines and chemokines. These effects on soluble mediators of inflammation can be significantly abrogated by LKB1 siRNAs, indicating that ETC-1002 activates AMPK and exerts its anti-inflammatory effects via an LKB1-dependent mechanism.
|In vivo||In vivo, ETC-1002 suppresses thioglycollate-induced homing of leukocytes into mouse peritoneal cavity. Similarly, 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. ETC-1002 is an inactive prodrug and converted to an active ACL inhibitor(ECT-1002-CoA) by endogenous liver ACS activity in vivo.|
|In vitro||DMSO||68 mg/mL (197.39 mM)|
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
|Synonyms||Bempedoic acid, ESP-55016|
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02659397||Completed||Drug: ETC-1002|Drug: Atorvastatin|Drug: Placebo||Hyperlipidemia||Esperion Therapeutics||December 2015||Phase 2|
|NCT02072161||Completed||Drug: ETC-1002|Drug: Placebo|Drug: Statin Therapy||Hypercholesterolemia||Esperion Therapeutics|Medpace Inc.||March 2014||Phase 2|
|NCT02044627||Completed||Drug: [14C-ETC-1002]||Hyperlipidemia||Esperion Therapeutics||December 2013||Phase 1|
|NCT01607294||Completed||Drug: ETC-1002|Drug: Placebo||Hyperlipidemia|Type 2 Diabetes||Esperion Therapeutics||April 2012||Phase 2|
|NCT01485146||Completed||Drug: ETC-1002||Safety Evaluation of Escalating Doses||Esperion Therapeutics||October 25 2011||Phase 1|
|NCT01262638||Completed||Drug: ETC-1002|Drug: Placebo||Dyslipidemia||Esperion Therapeutics||December 2010||Phase 2|
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