Norelgestromin

诺孕酯的活性代谢物；孕酮受体和ERα的激动剂（EC50s分别为11.1和43.4nM）；糖皮质激素和盐皮质激素受体的拮抗剂（IC50s分别为255nM和83.7nM）；选择性结合孕激素受体（兔子宫受体的IC50=4.61nM）而非雄激素受体（大鼠前列腺受体的IC50=222nM）；在表达人类受体的MDA-MB-231细胞的转录激活试验中激活雄激素受体。An active metabolite of norgestimate; an agonist of the progesterone receptor and ERα (EC50s= 11.1 and 43.4 nM, respectively); an antagonist of the glucocorticoid and mineralocorticoid receptors (IC50s = 255 nM and 83.7 nM, respectively); selectively binds progestin receptors (IC50 = 4.61 nM for rabbit uterine receptors) over androgen receptors (IC50 = 222 nM for rat prostatic receptors); activates the androgen receptor in a transactivation assay in MDA-MB-231 cells expressing the human receptor.分子式C21H29NO2分子量327.5CC[C@@]12[C@](CC[C@@]2(O)C#C)([H])[C@]3([H])CCC4=C/C(CC[C@]4([H])[C@@]3([H])CC1)=N/O