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 treatmetn of prostate cancer.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Related Androgen Receptor Products|
GSK 2881078 is a selective androgen receptor modulator potentially for the treatment of cachexia. GSK 2881078 is a selective androgen receptor modulator (SARM) that is being evaluated for effects on muscle growth and strength in subjects with muscle wasting to improve their physical function.
Indacaterol(Onbrez; Arcapta) is an ultra-long-acting β-adrenoceptor agonist.
Nandrolone phenylpropionate (NPP) is an anabolic-androgenic steroid. The low androgenicity and enhanced anabolic activity of NPP has shown to positively influence calcium metabolism and to increase bone mass in osteoporosis.
Testosterone is normally present in the circulation of both men and women. Due to the dynamic regulation of endogenous testosterone production, including the acute effects of competition and exercise, testosterone concentrations may vary considerably within and among individuals.
Testosterone phenylpropionate is a synthetic anabolic-androgenic steroid (AAS) and an androgen ester.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.