生物活性

Nilutamide (Nilandron, Anandron, RU 23908) is an androgen receptor (AR) blocker with an IC50 of 0.4 μM. The twofold stimulation of Shionogi cell proliferation caused by a 10-day exposure to 1 nM testosterone is competitively reversed by incubation with Nilutamide, at the IC50. Nilutamide at the IC50 values of 87 nM and in T-47D and ZR-75-1 cells blocks the marked increase in GCDFP-15 release induced by 1 nM testosterone.Nilutamide blocks the androgen induction of CYP27A1. Treatment of the HepG2 cells with dihydrotestosterone in presence of the AR antagonist Nilutamide almost completely abolishes the dihydrotestosterone-induced effect on the CYP27A1 promoter activity. Incubation with 100 μg/mL Nilutamide results in decreased movement of S. mansoni adults. Nilutamide inhibits hepatic cytochrome P-450 activity. Total worm burden reductions of 5.1%–35.6% are achieved with Nilutamide. The highest female worm burden reduction of 75.4% is observed with a 200 mg/kg dose of Nilutamide, while moderate female worm burden reductions of 22.5%–27.5% are observed following 50 mg/kg, 100 mg/kg and 400 mg/kg Nilutamide doses. At 400 mg/kg, Nilutamide reduced total and female worm burdens by 84.8% and 71.3%, respectively. Combinations of Nilutamide (100 mg/kg) and praziquantel (50 mg/kg  or 100 mg/kg) reveals an increase in worm survival, above the level observed with praziquantel or Nilutamide monotherapy. However, a combination of Nilutamide (200 mg/kg) and praziquantel (100 mg/kg) produces statistically significant total and female worm burden reductions by 90.6% and 85.1%, respectively. Anandron (20 mg/kg/day) with even low doses of buserelin leads to an immediate decrease in prostate weight that is complete at 15 days. Nilutamide and Dasatinib has entered in a phase II clinical trial in the treatment of prostate cancer. Nilutamide plus bicalutamide, buserelin, cyproterone acetate, flutamide, goserelin or leuprolide acetate has entered in a phase III clinical trial in the treatme

化学数据

不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

例如，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的K_m系数（3），再除以大鼠的K_m系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。

储备液配制

以下数据基于产品分子量，对于特殊产品，请参照COA中的储备液配制条件和说明进行操作。