Kelly, Martha J. published the artcileDiscovery 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, Related Products of bromides-buliding-blocks, the main research area is tetrahydrotriazinecarbonitrile derivative MGL3196 thyroid hormone receptor agonist dyslipidemia treatment.
The beneficial effects of thyroid hormone (TH) on lipid levels are primarily due to its action at the thyroid hormone receptor β (THR-β) in the liver, while adverse effects, including cardiac effects, are mediated by thyroid hormone receptor α (THR-α). A pyridazinone series has been identified that is significantly more THR-β selective than earlier analogs. Optimization of this series by the addition of a cyanoazauracil substituent improved both the potency and selectivity and led to MGL-3196 (53), which is 28-fold selective for THR-β over THR-α in a functional assay. Compound 53 showed outstanding safety in a rat heart model and was efficacious in a preclin. model at doses that showed no impact on the central thyroid axis. In reported studies in healthy volunteers, 53 exhibited an excellent safety profile and decreased LDL cholesterol (LDL-C) and triglycerides (TG) at once daily oral doses of 50 mg or higher given for 2 wk.
Journal of Medicinal Chemistry published new progress about Anticholesteremic agents. 74896-66-5 belongs to class bromides-buliding-blocks, name is Methyl 3,5-dibromo-4-methylbenzoate, and the molecular formula is C9H8Br2O2, Related Products of bromides-buliding-blocks.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary