NH-3 is an orally active, reversible thyroid hormone receptor (THR) antagonist with an IC 50 of 55 nM. NH-3, a derivative of the selective thyromi-metic GC-1, inhibits binding of thyroid hormones to their receptor and that inhibits cofactor recruitment.
性状
Solid
IC50 & Target[1][2]
IC50: 55 nM (THR)
体内研究(In Vivo)
NH3 (46.2-27,700 nmol/kg/day; 7 days) decreases heart rate modestly starting at 46.2 nmol/kg/day, but the effect was lost at >2920 nmol/kg/day. NH3 has no effect on the cholesterol-lowering action of 46.2 nmol/kg/day T3, but it inhibits the tachycardic and TSH suppressant effects up to the 924 nmol/kg/day dose. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Latika Singh, et al. Chasing the Elusive Benzofuran Impurity of the THR Antagonist NH-3: Synthesis, Isotope Labeling, and Biological Activity. J Org Chem. 2016 Mar 4;81(5):1870-6.[2]. Gary J Grover, et al. Pharmacological profile of the thyroid hormone receptor antagonist NH3 in rats. J Pharmacol Exp Ther. 2007 Jul;322(1):385-90.
溶解度数据
In Vitro: DMSO : 100 mg/mL (211.18 mM; Need ultrasonic)配制储备液