ETC-1002

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].

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]	+ Expand 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]	+ Expand Animal Models: C57BL/6 male mice Formulation: A disodium salt aqueous solution using 2:1 molar ratio of NaOH to ETC-1002 in water containing 0.5% CMC and 0.025% Tween with a final pH 7–8. Dosages: 10 ml/kg Administration: i.p. (Only for Reference)

Cell Research:

^[2]

+ Expand

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]

+ Expand

Animal Models: C57BL/6 male mice
Formulation: A disodium salt aqueous solution using 2:1 molar ratio of NaOH to ETC-1002 in water containing 0.5% CMC and 0.025% Tween with a final pH 7–8.
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

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Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2018-10-19)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT03531905	Recruiting	Diabetes\|Diabetes Mellitus Type 2\|Cholesterolemia	Esperion Therapeutics	May 9 2018	Phase 2
NCT03193047	Completed	Hypercholesterolemia	Esperion Therapeutics	April 7 2017	Phase 2
NCT03067441	Active not recruiting	Hypercholesterolemia\|Atherosclerotic Cardiovascular Disease	Esperion Therapeutics	February 3 2017	Phase 3
NCT03001076	Completed	Hypercholesterolemia\|Atherosclerosis\|Statin Adverse Reaction	Esperion Therapeutics	November 29 2016	Phase 3
NCT03337308	Completed	Hyperlipidemias	Esperion Therapeutics	October 23 2017	Phase 3
NCT02993406	Recruiting	Cardiovascular Diseases\|Statin Adverse Reaction	Esperion Therapeutics\|The Cleveland Clinic	December 2016	Phase 3

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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AMPK Signaling Pathway Map

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ETC-1002

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Biological Activity

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References

Solubility (25°C)

Chemical Information Download ETC-1002 SDF

Bio Calculators

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Dilution Calculator

Concentration _(start) x Volume _(start) = Concentration _(final) x Volume _(final)

The Serial Dilution Calculator Equation

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Total Molecular Weight: g/mol

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Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2018-10-19)

Tech Support

AMPK Signaling Pathway Map

Related AMPK Products

Choose Your Country or Region

By Signaling Pathways

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ETC-1002

Purity & Quality Control

Choose Selective AMPK Inhibitors

Biological Activity

Protocol

References

Solubility (25°C)

Chemical Information Download ETC-1002 SDF

Bio Calculators

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Dilution Calculator

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

The Serial Dilution Calculator Equation

Serial Dilutions

Computed Result

Molecular Weight Calculator

Total Molecular Weight: g/mol

Instructions to calculate molar mass (molecular weight) of a chemical compound:

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molarity Calculator

Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2018-10-19)

Tech Support

AMPK Signaling Pathway Map

Related AMPK Products

Concentration _(start) x Volume _(start) = Concentration _(final) x Volume _(final)