Finasteride is a potent, reversible inhibitor of the rat type 1 5 alpha-reductase with Ki of 10.2 nM, used in the treatment of benign prostatic hyperplasia (BPH) and male pattern baldness (MPB).
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产品名称 | 5-alpha Reductase ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
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Dutasteride | ✔ | 98% | |||||||||||||||||
Finasteride |
+++
5-α reductase, Ki: 10.2 nM |
98% | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
靶点 |
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描述 | Steroid 5α-reductase (5αR) is the NADPH-dependent enzyme required for the conversion of testosterone (T) to dihydrotestosterone (DHT) [7]. Finasteride is an orally active testosterone 5-α-reductase inhibitor (Ki= 10 nM) [8]. In COS cells expressing rat types 1 or 2 5αR, finasteride displays reversible inhibition of rat type 1 5αR and time-dependent inhibition of rat type 2 5αR, and it is a potent inhibitor of both isozymes with IC50 values of 13 nM and 1 nM, respectively [7]. The growth rate of the LnCap cell line can be dose-dependently inhibited by finasteride in vitro, in defined conditions [9]. Binding of LNCaP cell nuclear proteins to steroid receptor-binding consensus (SRBC) was diminished when the cells were exposed to 25 microM finasteride, at which concentration 50% of both prostate-specific antigen (PSA) mRNA and protein were inhibited [10]. Finasteride treatment induced dosage-related incidences of hypospadias (penischisis) in male offspring with a threshold dosage level near 0.1 mg/kg/day and a 100% effect level of 100 mg/kg/day (with dosing through Day 20 of gestation) [11]. |
Animal study | 尿道下裂模型 动物:SD大鼠,雌雄皆有,SPF级, 体重: ~150 g。 给药:雌鼠受孕第8天灌胃非那雄胺,1周后成功制备尿道下裂模型。 |
Pharmacokinetics |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.68mL 0.54mL 0.27mL |
13.42mL 2.68mL 1.34mL |
26.84mL 5.37mL 2.68mL |
CAS号 | 98319-26-7 |
分子式 | C23H36N2O2 |
分子量 | 372.54 |
别名 | 非那甾胺 ;MK-906 |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,Store in freezer, under -20°C |
溶解度 |
DMSO: 145 mg/mL(389.22 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |
IP 2% DMSO+2% Tween80+40% PEG300+water 7 mg/mL clear PO 0.5% CMC-Na 40 mg/mL suspension |