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.
性状
Solid
IC50 & Target[1][2]
Androgen receptor, Parasite
体外研究(In Vitro)
Nilutamide (110 μM) inhibits hexobarbital hydroxylase, benzphetamine N-demethylase, benzo(a)pyrene hydroxylase and 7-ethoxycoumarin O-deethylase activities by 85, 40, 35 and 25%, respectively, in human liver microsomes.Nilutamide (550 μM) does not significantly increase the consumption of NADPH by aerobic microsomes, and does not modify the kinetics for the reduction of cytochrome P-450 by NADPH-cytochrome P-450 reductase in an anaerobic system.Nilutamide blocks the marked increase in GCDFP-15 release induced by 1 nM testosterone in T-47D cells and ZR-75-1 cells with IC50s of 87 nM and 75 nM, respectively. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Nilutamide (50-400 mg/kg; p.o.; single dosage) reduces juvenile and adult Schistosoma mansoni cercariae worm burdens in infected mice. has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[1]. Harris MG, et al. Nilutamide. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in prostate cancer. Drugs Aging. 1993 Jan-Feb;3(1):9-25.[2]. Babany G, et al. Inhibitory effects of nilutamide, a new androgen receptor antagonist, on mouse and human liver cytochrome P-450. Biochem Pharmacol. 1989 Mar 15;38(6):941-7.