| Bioactivity | 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]. | ||||||||||||
| Target | IC50: 55 nM (THR) | ||||||||||||
| 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[2]. | ||||||||||||
| Name | NH-3 | ||||||||||||
| CAS | 447415-26-1 | ||||||||||||
| Formula | C28H27NO6 | ||||||||||||
| Molar Mass | 473.52 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. [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. |