447415-26-1

NH-3 is an orally active, reversible thyroid hormone receptor (THR) antagonist with an IC50 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[1][2][3]. NH-3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

[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. DOI:10.1021/acs.joc.5b02665
[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. DOI:10.1124/jpet.106.116152
[3] Wayland Lim, et al. A thyroid hormone antagonist that inhibits thyroid hormone action in vivo. J Biol Chem. 2002 Sep 20;277(38):35664-70. DOI:10.1074/jbc.M205608200