Finasteride (MK-906) 是一种有效的竞争性 5α-还原酶 (5α-reductase) 抑制剂，对 II 型 5α-还原酶的IC50值为 4.2 nM。Finasteride 对 II 型 5α-还原酶的亲和力比对 I 型酶高约 100 倍。Finasteride 可用于研究前列腺增生 (BPH) 和雄激素性脱发。
| 生物活性 | Finasteride (MK-906) is a potent and competitive5α-reductaseinhibitor, with anIC50of 4.2 nM for type II 5α-reductase. Finasteride has approximately a 100-fold greater affinity for type II 5α-reductase enzyme than for the type I enzyme. Finasteride can be used for the research of benign prostatic hyperplasia (BPH) and androgenic alopecia[1][2][3]. |
| IC50& Target | IC50: 4.2 nM (type II 5α-reductase)[1] |
体外研究
(In Vitro) | Finasteride (10 μM; 6-24 h) induces the expression of HO-1 and Nrf2 proteins in PC-3 cells[2].
Finasteride decreases the conversion of [3H]testosterone (T) to [3H]dihydrotestosterone (DHT) inP. crustosum[1].
Western Blot Analysis[2] | Cell Line: | PC-3, DU-145, and LNCaP cells | | Concentration: | 10 μM | | Incubation Time: | 6, 12, 24 h | | Result: | Increased the expression of HO-1 protein in a time-dependent manner in PC-3 cells.
Induced the expression of Nrf2 protein in DU-145 and PC-3 cells, but not in LNCaP cells. |
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体内研究
(In Vivo) | Finasteride (0.1-0.5 mg/kg; p.o. once daily for 16 weeks) reduces prostatic size in dogs with BPH without adversely affecting semen quality or serum testosterone concentration[3].
| Animal Model: | Male dogs with spontaneous BPH (2.7-11 years old; 10.3-49 kg)[3] | | Dosage: | 0.1-0.5 mg/kg | | Administration: | P.o. once daily for 16 weeks | | Result: | Decreased prostatic diameter (20%), prostatic volume (43%), and serum DHT concentration (58%).
Decreased semen volume but did not adversely effect on semen quality or serum testosterone concentration.
No adverse effects on dogs. |
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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 : 150 mg/mL(402.64 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.6843 mL | 13.4214 mL | 26.8428 mL | | 5 mM | 0.5369 mL | 2.6843 mL | 5.3686 mL | | 10 mM | 0.2684 mL | 1.3421 mL | 2.6843 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 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (6.71 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.71 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 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。 2. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (6.71 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.71 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 3. 请依序添加每种溶剂： 50%PEG300 50% saline Solubility: 2 mg/mL (5.37 mM); Suspended solution; Need ultrasonic
*以上所有助溶剂都可在本网站选购。 |
