Sobetirome

TRβ激动剂（报告分析中EC50=7nM）；选择性结合TRβ而非TRα（Kds分别为0.1和1.8nM）；在以97nmol/kg剂量喂食正常食物或高胆固醇饮食的小鼠中，可提高肝脏SR-B1水平和血清C4水平；在这些模型中，可降低血清胆固醇和甘油三酯水平；在以154nmol/kg剂量喂食含有5-丙基-2-硫代尿嘧啶的缺碘饮食诱发的甲状腺功能减退症小鼠模型中，可降低血浆胆固醇水平。A TRβ agonist (EC50 = 7 nM in a reporter assay); selectively binds to TRβ over TRα (Kds = 0.1 and 1.8 nM, respectively); increases hepatic SR-B1 levels and serum C4 levels in mice fed normal chow or high-cholesterol diets at 97 nmol/kg; reduces serum cholesterol and triglyceride levels in these same models; decreases plasma cholesterol levels in a mouse model of hypothyroidism induced by an iodine-deficient diet containing 5-propyl-2-thio-uracil at 154 nmol/kg.分子式C20H24O4分子量328.4OC1=C(C(C)C)C=C(CC2=C(C)C=C(OCC(O)=O)C=C2C)C=C1