Bempedoic acid (ETC-1002)

Synonyms: ESP-55016

Bempedoic acid (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).

Bempedoic acid (ETC-1002) Chemical Structure

Bempedoic acid (ETC-1002) Chemical Structure

CAS: 738606-46-7

Selleck's Bempedoic acid (ETC-1002) has been cited by 4 publications

Purity & Quality Control

Batch: S795301 DMSO] 68 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.13%
99.13

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Signaling Pathway

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Biological Activity

Description Bempedoic acid (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).
Targets
AMPK [1]
In vitro
In vitro 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[1]. 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[2].
Cell Research Cell lines Primary rat hepatocytes and differentiated human monocyte-derived macrophages
Concentrations 30 μM or 100 μM
Incubation Time 12 h
Method

Primary rat hepatocytes and differentiated human MDMs are treated with indicated concentrations of ETC-1002 for 12 h. Working solutions of ETC-1002 are prepared in serum-free RPMI 1640 containing 12 mM HEPES, 10,000 U/ml penicillin, and 100 μg/ml streptomycin.

Experimental Result Images Methods Biomarkers Images PMID
Western blot p-ACC / ACC / p-AMPK / AMPK / p-HMGR 23118444
In Vivo
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[2]. ETC-1002 is an inactive prodrug and converted to an active ACL inhibitor(ECT-1002-CoA) by endogenous liver ACS activity in vivo[3].
Animal Research Animal Models C57BL/6 male mice
Dosages 10 ml/kg
Administration i.p.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05694260 Recruiting
Hypercholesterolemia
Esperion Therapeutics Inc.
January 12 2023 Phase 2
NCT04929249 Completed
Atherosclerotic Cardiovascular Disease
Novartis Pharmaceuticals|Novartis
June 25 2021 Phase 3
NCT02659397 Completed
Hyperlipidemia
Esperion Therapeutics Inc.
December 2015 Phase 2
NCT02178098 Completed
Hypercholesterolemia|Hypertension
Esperion Therapeutics Inc.|Medpace Inc.
June 16 2014 Phase 2

Chemical Information & Solubility

Molecular Weight 344.49 Formula

C19H36O5

CAS No. 738606-46-7 SDF Download Bempedoic acid (ETC-1002) SDF
Smiles CC(C)(CCCCCC(CCCCCC(C)(C)C(=O)O)O)C(=O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 68 mg/mL ( (197.39 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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