Free shipping on all orders over $ 500

ETC-1002

Cat. No. M5207
ETC-1002 Structure
Synonym:

ESP-55016

Size Price Availability Quantity
5mg USD 120 In stock
10mg USD 200 In stock
Bulk Inquiry?

Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

ETC-1002 mediates inhibition of a wide range of proinflammatory molecules that coincides with the modulation of AMPK and MAP kinase activities. It has potent inhibitory activity against hepatic ATP-citrate lyase(IC50=29 uM).

In vitro: The phospho-ACC to total-ACC ratio increased by 25% and 60% in cells treated with 50 µM and 100 µM ETC-1002, respectively.ETC-1002 has AMPK-activating properties in primary human MDMs.

In vivo: when mice were treated with 30 mg/kg of ETC-1002 prior to thioglycollate administration, leukocyte influx into the peritoneal cavity was significantly reduced by 48% at 24 h (13.7 × 106/ml lavage fluid; P < 0.008) and by 61% at 72 h (1.8 × 106/ml lavage fluid; P < 0.002)

Protocol
Cell Experiment
Cell lines Primary rat hepatocytes and differentiated human monocyte-derived macrophages
Preparation 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.
Concentrations 30 μM or 100 μM
Incubation time 12 h
Animal Experiment
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.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 344.49
Formula C19H36O5
CAS Number 738606-46-7
Purity >99%
Solubility DMSO 60 mg/mL
Storage at -20°C
References

ETC-1002: a future option for lipid disorders?
Nikolic D, et al. Atherosclerosis. 2014 Dec;237(2):705-10. PMID: 25463109.

ETC-1002 regulates immune response, leukocyte homing, and adipose tissue inflammation via LKB1-dependent activation of macrophage AMPK.
Filippov S, et al. J Lipid Res. 2013 Aug;54(8):2095-108. PMID: 23709692.

Related AMPK Products
Phenformin HCl

Phenformin HCl is a hydrochloride salt of phenformin that is an anti-diabetic drug from the biguanide class. It activates AMPK, increasing activity and phosphorylation.

HTH-01-015

HTH-01-015 is a potent and selective NUAK1 inhibitor with IC50 of 100 nM, >100-fold selectivity over NUAK2.

AICAR

AICAR is an activator of AMP-activated protein kinase (AMPK), down-regulates the insulin receptor expression in HepG2 cells.

BML-275

BML-275 (Dorsomorphin) is a cell-permeable pyrazolopyrimidine compound shown to be an AMPK inhibitor with Ki of 109 nM in cell-free assays.

A-769662

A-769662 is a potent, reversible AMPK activator with EC50of 0.8 μM, little effect on GPPase/FBPase activity.

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: ETC-1002, ESP-55016 supplier, AMPK, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.