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)
|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 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|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Solubility||DMSO 60 mg/mL|
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.
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