AC-262536

SARM（Ki=5.01nM）；雄激素受体部分激动剂（在荧光素酶测定中EC50=1.58nM）；在10µM浓度下，对47种其他人类核受体中的雄激素受体具有选择性；在0.1和1µM浓度下抑制二羟睾酮诱导的LNCaP前列腺癌细胞增殖；在3、10和30mg/kg浓度下，降低去势大鼠血浆促黄体生成素水平，增加肛提肌重量；与同一模型中的睾酮相比，前列腺和精囊重量的增加幅度较小。A SARM (Ki = 5.01 nM); an androgen receptor partial agonist (EC50 = 1.58 nM in a luciferase assay); selective for the androgen receptor over a panel of 47 additional human nuclear receptors at 10 µM; inhibits dihydroxytestosterone-induced proliferation of LNCaP prostate cancer cells at 0.1 and 1 µM; reduces plasma luteinizing hormone levels and increases levator ani muscle weight in castrated rats at 3, 10, and 30 mg/kg; exhibits smaller increases in prostate gland and seminal vesicle weight compared with testosterone in the same model.分子式C18H18N2O分子量278.4O[C@@H]1C[C@H]2N(C3=CC=C(C#N)C4=C3C=CC=C4)[C@@H](C1)CC2