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
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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Form:Solid
IC50& Target:IC50: 55 nM (THR)
规格
规格或纯度
≥98%
英文名称
NH-3
生化机理
NH-3 是一种口服活性、可逆的甲状腺激素受体(THR)拮抗剂,其 IC 50 为 55 nM。NH-3 是选择性甲状腺激素受体 GC-1 的衍生物,可抑制甲状腺激素与其受体的结合,并抑制辅助因子的招募[1]。