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编 号:F413042
分子式:C12H10F3N3O4
分子量:317.22
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10mM*1mL in DMSO
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100mg
349
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生物活性:
Nilutamide (Nilandron) is an orally active nonsteroidal androgen receptor antagonist with affinity for androgen receptors but not for progestogen, estrogen or glucocorticoid receptors. Nilutamide can be used to research prostate cancer. Nilutamide also has antischistosomal properties.

体内研究:
Nilutamide (50-400 mg/kg;口服;单剂量) 减少受感染小鼠中幼年和成年曼氏血吸虫尾蚴蠕虫负担。Animal Model:Female NMRI mice (20-22 g; n=165; infected subcutaneously with ~80 Schistosoma mansoni cercariae)
Dosage:50, 100, 200 and 400 mg/kg
Administration:p.o.; single dosage ( 21- or 49-day-old S. mansoni infection)
Result:Reduced total juvenile worm burden with 11.0%, 5.1%, 21.9% and 35.6% at 50, 100, 200 and 400 mg/kg, respectively.Reduced female juvenile worm with 27.5%, 26.1%, 75.4% and 22.5% at 50, 100, 200 and 400 mg/kg, respectively.Observed moderate adult worm reduction with 30.7%-49.6% at 100 and 200 mg/kg.Reduced total and female adult worm burdens by 84.8% and 71.3%, respectively, at 400 mg/kg.

体外研究:
Nilutamide (110 μM) 在人肝微粒体中分别抑制六巴比妥羟化酶、苯丙胺 N-脱甲基酶、苯并 (a) 芘羟化酶和 7-乙氧基香豆素 O-脱乙基酶活性 85%、40%、35% 和 25%。 Nilutamide (550 μM) 不会显著增加需氧微粒体对 NADPH 的消耗,也不会改变 NADPH-细胞色素 P-450 还原酶在 NADPH 中还原细胞色素 P-450 的动力学厌氧系统。 Nilutamide 阻断 T-47D 细胞和 ZR-75-1 细胞中 1 nM 睾酮诱导的 GCDFP-15 释放显著增加,IC50分别为 87 nM 和 75 nM。
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