An agonist of TRβ
Animal experiment: | Rats[1]Resmetirom (MGL-3196), compounds 54 and 55 are formulated in 4% DMSO, 15% PEG-400, and 81% of 30% HPBCD in phosphate buffer and are administered intraperitoneally. For MGL-3196 and 54, 4 rats per group are tested at 5, 20, and 37.5 mg/kg. For 55, 3 rats per group are tested at 5 and 15 mg/kg and 4 rats are tested at 50 mg/kg[1]. Mice[1]Six week old C57Bl/6J mice are placed on a high fat diet for 34 weeks. At day 0, 9 mice per group are treated daily doses by gavage with vehicle (2% Klucel LF, 0.1% Tween 80 in water) or 0.3, 1, 3, or 10 mg/kg Resmetirom (MGL-3196) for 23 days. In a parallel study, at day 0, 9 mice per group are treated with daily doses of vehicle (Dulbecco’s phosphate buffered saline, pH adjusted to 9.0 with 1 N NaOH) or 10, 30, or 100 μg/kg T3[1]. |
参考文献: [1]. Kelly MJ, et al. Discovery of 2-[3,5-dichloro-4-(5-isopropyl-6-oxo-1,6-dihydropyridazin-3-yloxy)phenyl]-3,5-dioxo-2,3,4,5-tetrahydro[1,2,4]triazine-6-carbonitrile (MGL-3196), a Highly Selective Thyroid Hormone Receptor β agonist in clinical trials for the treatment of dyslipidemia. J Med Chem. 2014 May 22;57(10):3912-23. | |
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