PeptideDB

Nilutamide

CAS: 63612-50-0 F: C12H10F3N3O4 W: 317.22

Nilutamide (Nilandron) is an orally active nonsteroidal androgen receptor antagonist with affinity for androgen receptor
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This product is for research use only, not for human use. We do not sell to patients.

Bioactivity 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[1][4].
Target Androgen receptor, Parasite
Invitro 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[2].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[2].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[3].
In Vivo Nilutamide (50-400 mg/kg; p.o.; single dosage) reduces juvenile and adult Schistosoma mansoni cercariae worm burdens in infected mice[4]. Animal Model:
Name Nilutamide
CAS 63612-50-0
Formula C12H10F3N3O4
Molar Mass 317.22
Appearance Solid
Transport Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Reference [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. [3]. Simard J, et al. Comparison of in vitro effects of the pure antiandrogens OH-flutamide, Casodex, and nilutamide on androgen-sensitive parameters. Urology. 1997 Apr;49(4):580-6; discussion 586-9. [4]. Keiser J, Vargas M, Vennerstrom JL. Activity of antiandrogens against juvenile and adult Schistosoma mansoni in mice. J Antimicrob Chemother. 2010 Sep;65(9):1991-5.