1. Epigenetics
    PI3K/Akt/mTOR
  2. AMPK

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

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

ETC-1002 is an activator of hepatic AMP-activated protein kinase (AMPK).

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

ETC-1002 Chemical Structure

ETC-1002 Chemical Structure

CAS No. : 738606-46-7

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
5 mg USD 60 In-stock
Estimated Time of Arrival: December 31
10 mg USD 90 In-stock
Estimated Time of Arrival: December 31
50 mg USD 270 In-stock
Estimated Time of Arrival: December 31
100 mg USD 450 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

ETC-1002 is an activator of hepatic AMP-activated protein kinase (AMPK).

IC50 & Target[1]

AMPK

 

In Vitro

ETC-1002 free acid 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. ETC-1002 is shown to rapidly form a CoA thioester in liver, which directly inhibits ATP-citrate lyase[1]. In cells treated with 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 ETC-1002. ETC-1002 free acid is >100-fold more prevalent than the CoA thioester in rat liver and is associated with AMPK activation[1]. ETC-1002 suppresses thioglycollate-induced homing of leukocytes into mouse peritoneal cavity. 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].

Clinical Trial
Solvent & Solubility
In Vitro: 

10 mM in DMSO

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.
References
Kinase Assay
[1]

7.5× compounds are added to a 96-well PolyPlate containing 60 μL of Buffer per well with substrates CoA (200 μM), ATP (400 μM), and [14C]citrate. Reaction is started with 4 μL (300 ng/well) ACL, and the plate is incubated at 37°C for 3 h. Th

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

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 and without 0.3 μM glucagon with various concentrations of ETC-1002 (0.1 to 100 μM). Cells are washed twice in GPB. Cells are then incubated for an additional hour to assess glucose production by adding GPB containing equivalent glucagon concentrations without ETC-1002. Cells are incubated for 1 h, and the concentration of glucose in the media is determined[1].

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

Animal Administration
[1]

Rats: Prior to single-dose ETC-1002 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 ETC-1002 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 ETC-1002 [1].

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

References
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

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Purity: >98.0%

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Product Name:
ETC-1002
Cat. No.:
HY-12357
Quantity:

ETC-1002

Cat. No.: HY-12357