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。
| 生物活性 | Nilutamide (Nilandron) is an orally active nonsteroidalandrogen receptorantagonist with affinity for androgen receptors but not for progestogen, estrogen or glucocorticoid receptors. Nilutamide can be used to research prostatecancer. Nilutamide also has antischistosomal properties[1][4]. |
| IC50& Target | Androgen receptor, Parasite[1][4] |
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[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].
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体内研究
(In Vivo) | Nilutamide (50-400 mg/kg; p.o.; single dosage) reduces juvenile and adultSchistosoma mansoni cercariaeworm burdens in infected mice[4].
| Animal Model: | Female NMRI mice (20-22 g; n=165; infected subcutaneously with ~80Schistosoma mansoni cercariae)[4] | | Dosage: | 50, 100, 200 and 400 mg/kg | | Administration: | p.o.; single dosage ( 21- or 49-day-oldS. mansoniinfection) | | 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.
Reduced total and female adult worm burdens by 84.8% and 71.3%, respectively, at 400 mg/kg. |
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| 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 | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : ≥ 250 mg/mL(788.10 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 3.1524 mL | 15.7619 mL | 31.5239 mL | | 5 mM | 0.6305 mL | 3.1524 mL | 6.3048 mL | | 10 mM | 0.3152 mL | 1.5762 mL | 3.1524 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (6.56 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (6.56 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (6.56 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (6.56 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (6.56 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (6.56 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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