Nilutamide

SKU: orb1224392

Description

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.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 63612-50-0
• MW: 317.22
• Purity: >98% (HPLC)
• Formula: C₁₂H₁₀F₃N₃O₄
• SMILES: O=C1N(C2=CC=C([N+]([O-])=O)C(C(F)(F)F)=C2)C(C(C)(C)N1)=O
• Target: Androgen Receptor (AR)
• Solubility: DMSO: 10 mM

Bioactivity

• In Vivo:
  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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

RU-23908

Quick Database Links

Gene Symbol

Androgen Receptor (AR)