Finasteride(Synonyms: 非那雄胺; MK-906)

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Finasteride (Synonyms: 非那雄胺; MK-906) 纯度: 99.97%

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。

Finasteride(Synonyms: 非那雄胺; MK-906)

Finasteride Chemical Structure

CAS No. : 98319-26-7

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生物活性

Finasteride (MK-906) is a potent and competitive 5α-reductase inhibitor, with an IC50 of 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) in P. crustosum[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Clinical Trial

分子量

372.54

Formula

C23H36N2O2
CAS 号

98319-26-7
中文名称

非那雄胺；非那斯特萊；非那司提；非那甾胺
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
溶解性数据
In Vitro: 

DMSO : 150 mg/mL (402.64 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 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-CD in 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 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 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。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Flores E, et, al. Steroid 5alpha-reductase inhibitors. Mini Rev Med Chem. 2003 May;3(3):225-37.

    [2]. Yun DK, et, al. Finasteride Increases the Expression of Hemoxygenase-1 (HO-1) and NF-E2-Related Factor-2 (Nrf2) Proteins in PC-3 Cells: Implication of Finasteride-Mediated High-Grade Prostate Tumor Occurrence. Biomol Ther (Seoul). 2013 Jan;21(1):49-53.

    [3]. Sirinarumitr K, et, al. Effects of finasteride on size of the prostate gland and semen quality in dogs with benign prostatic hypertrophy. J Am Vet Med Assoc. 2001 Apr 15;218(8):1275-80.

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