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Bempedoic acid (ETC-1002) AMPK activator

Name: Bempedoic acid (ETC-1002)
Brand: Selleck Chemicals
SKU: S7953
Availability: InStock
Rating: 5 (5 reviews)

Cat.No.S7953

Bempedoic acid (ETC-1002) is an orally available, once-daily LDL-C lowering small molecule designed to reduce elevated levels of LDL-C and to avoid side effects associated with existing LDL-C lowering therapies. This compound is an activator of hepatic AMP-activated protein kinase (AMPK) and has potent inhibitory activity against hepatic ATP-citrate lyase(IC50=29 uM).

Chemical Structure

Molecular Weight: 344.49

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

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

99.13

Related Targets	PI3K Akt mTOR GSK-3 ATM/ATR DNA-PK PDPK1 PTEN PP2A PDK PI4K PIKfyve MELK
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Chemical Information, Storage & Stability

Molecular Weight	344.49	Formula	C₁₉H₃₆O₅	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	738606-46-7	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	ESP-55016			Smiles	CC(C)(CCCCCC(CCCCCC(C)(C)C(=O)O)O)C(=O)O

Solubility

In vitro
Batch:

DMSO : 68 mg/mL (197.39 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (14.51mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (14.51mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

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 μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, 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.

Mechanism of Action

Targets/IC₅₀/Ki	AMPK ^[1]
In vitro	Bempedoic acid (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 this compound activates AMPK and exerts its anti-inflammatory effects via an LKB1-dependent mechanism^[2].
In vivo	In vivo, Bempedoic acid (ETC-1002) suppresses thioglycollate-induced homing of leukocytes into mouse peritoneal cavity. Similarly, in a mouse model of diet-induced obesity, it restores adipose AMPK activity, reduces JNK phosphorylation, and diminishes expression of macrophage-specific marker 4F/80^[2]. This compound is an inactive prodrug and converted to an active ACL inhibitor(ECT-1002-CoA) by endogenous liver ACS activity in vivo^[3].
References	[1] https://pubmed.ncbi.nlm.nih.gov/25463109/ [2] https://pubmed.ncbi.nlm.nih.gov/23709692/ [3] https://pubmed.ncbi.nlm.nih.gov/23118444/

Applications

Methods	Biomarkers	Images	PMID
Western blot	p-ACC / ACC / p-AMPK / AMPK / p-HMGR		23118444

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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