1. Metabolic Enzyme/Protease
    PI3K/Akt/mTOR
    Epigenetics
  2. ATP Citrate Lyase
    AMPK
  3. Bempedoic acid

Bempedoic acid (Synonyms: ETC-1002; ESP-55016)

Cat. No.: HY-12357 Purity: >98.0%
Handling Instructions

Bempedoic acid (ETC-1002) is an ATP-citrate lyase (ACL) inhibitor. Bempedoic acid (ETC-1002) activates AMPK.

For research use only. We do not sell to patients.

Bempedoic acid Chemical Structure

Bempedoic acid Chemical Structure

CAS No. : 738606-46-7

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 61 In-stock
Estimated Time of Arrival: December 31
5 mg USD 55 In-stock
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10 mg USD 80 In-stock
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50 mg USD 270 In-stock
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100 mg USD 450 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

Bempedoic acid (ETC-1002) is an ATP-citrate lyase (ACL) inhibitor[1]. Bempedoic acid (ETC-1002) activates AMPK[2].

IC50 & Target[1]

AMPK

 

In Vitro

Bempedoic acid (ETC-1002) activates AMP-activated protein kinase in a Ca2+/calmodulin-dependent kinase β-independent and liver kinase β 1-dependent manner, without detectable changes in adenylate energy charge. Bempedoic acid is shown to rapidly form a CoA thioester in liver, which directly inhibits ATP-citrate lyase[1]. In cells treated with Bempedoic acid (ETC-1002), increased levels of AMP-activated protein kinase (AMPK) phosphorylation coincide with reduced activity of MAP kinases and decreased production of proinflammatory cytokines and chemokines[2].

In Vivo

A marked and sustained increase in AMPK and ACC phosphorylation is found in rat livers following two weeks of treatment with Bempedoic acid (ETC-1002). Bempedoic acid is >100-fold more prevalent than the CoA thioester in rat liver and is associated with AMPK activation[1]. Bempedoic acid (ETC-1002) suppresses thioglycollate-induced homing of leukocytes into mouse peritoneal cavity. In a mouse model of diet-induced obesity, Bempedoic acid restores adipose AMPK activity, reduces JNK phosphorylation, and diminishes expression of macrophage-specific marker 4F/80[2].

Clinical Trial
Molecular Weight

344.49

Formula

C₁₉H₃₆O₅

CAS No.

738606-46-7

SMILES

O=C(O)C(C)(C)CCCCCC(O)CCCCCC(C)(C)C(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (290.28 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9028 mL 14.5142 mL 29.0284 mL
5 mM 0.5806 mL 2.9028 mL 5.8057 mL
10 mM 0.2903 mL 1.4514 mL 2.9028 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (7.26 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (7.26 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (7.26 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[1]

Glucose production is measured in primary rat hepatocyte cultures. Cells are cultured in glucose- and phenol red-free DMEM, containing 10 mM lactate, 1 mM pyruvate, and nonessential amino acids. Cells are incubated with various concentrations of Bempedoic acid (0.1 to 100 μM)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Rats: Prior to single-dose Bempedoic acid administration, Male Wistar Han rats are fasted for 48 h and refed a high-carbohydrate diet for an additional 48 h. For two-week assessment, rats are maintained on standard chow diet and dosed by oral gavage with Bempedoic acid at 30 mg/kg/day for two weeks in the morning. Following nutritional staging and/or dosing, food is withdrawn 2 h prior to last the oral dose of ehicle control or Bempedoic acid[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: >98.0%

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Keywords:

Bempedoic acidETC-1002ESP-55016ETC1002ETC 1002ESP55016ESP 55016ATP Citrate LyaseAMPKACLYAMP-activated protein kinaseInhibitorinhibitorinhibit

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Bempedoic acid
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