Nilutamide

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Nilutamide (Nilandron) 是一种口服活性的非甾体雄激素受体拮抗剂，对雄激素受体有亲和力，但对孕激素、雌激素或糖皮质激素受体无亲和力。Nilutamide 可用于研究前列腺癌。Nilutamide 还具有抗血吸虫作用。

Nilutamide is an antineoplastic hormonal agent primarily used in the treatment of prostate Y. Nilutamide is a pure, nonsteroidal anti-androgen with affinity for androgen receptors (but not for progestogen, estrogen, or glucocorticoid receptors). Consequently, Nilutamide blocks the action of androgens of adrenal and testicular origin that stimulate the growth of normal and malignant prostatic tissue. Prostate Y is mostly androgen-dependent and can be treated with surgical or chemical castration. To date, antiandrogen monotherapy has not consistently been shown to be equivalent to castration. (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.(In Vivo):Nilutamide (50-400 mg/kg; p.o.; single dosage) reduces juvenile and adult Schistosoma mansoni cercariae worm burdens in infected mice.

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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.

RU-23908

Endocrinology/Hormones

Androgen Receptor (AR)

Androgen Receptor

Cancer

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63612-50-0

317.22

C12H10F3N3O4

>98% (HPLC)

DMSO: 10 mM

O=C1N(C2=CC=C([N+]([O-])=O)C(C(F)(F)F)=C2)C(C(C)(C)N1)=O

5,5-dimethyl-3-(4-nitro-3-(trifluoromethyl)phenyl)imidazolidine-2,4-dione

(-20℃)

With Ice Pack

≥ 2 years