ETC-1002

Name: ETC-1002
Brand: Selleck Chemicals
SKU: S7953
Rating: 5 (0 reviews)

For research use only.

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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Biological Activity

Description

Targets

AMPK ^[1]
()

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].

Assay

Methods	Test Index	PMID
Western blot	p-ACC / ACC / p-AMPK / AMPK / p-HMGR ; PubMed: 23118444 J Lipid Res AMPK (T172), ACC (S79), and HMGR (S872) phosphorylation was measured in primary rat hepatocytes treated with 30 μM ETC-1002 for the indicated times.	23118444

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].

Protocol

Cell Research:

^[2]

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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.

(Only for Reference)

Animal Research:

^[2]

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Animal Models: C57BL/6 male mice
Dosages: 10 ml/kg
Administration: i.p.
(Only for Reference)

References

Solubility (25°C)

In vitro	DMSO	68 mg/mL (197.39 mM)
	Water	Insoluble
	Ethanol	Insoluble

* 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.

Chemical Information Download ETC-1002 SDF

Molecular Weight	344.49
Formula	C₁₉H₃₆O₅
CAS No.	738606-46-7
Storage	3 years -20°C powder
Storage	2 years -80°C in solvent
Synonyms	Bempedoic acid, ESP-55016
Smiles	CC(C)(CCCCCC(O)CCCCCC(C)(C)C(O)=O)C(O)=O

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Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL， Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH₂O，mix and clarify.

Note：1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Bio Calculators

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Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2020-05-15)

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

Tech Support

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.

Handling Instructions

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