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Finasteride

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Chemical Structure| 98319-26-7 同义名 : 非那甾胺 ;MK-906
CAS号 : 98319-26-7
货号 : A201116
分子式 : C23H36N2O2
纯度 : 98%
分子量 : 372.54
MDL号 : MFCD00869737
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
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

生物活性
靶点

  • 5-alpha Reductase

    5-α reductase, Ki:10.2 nM
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].
作用机制 It is now clear that the mechanism of inhibition of the 5αRs involves reduction of the A-ring of the azasteroid and subsequent adduct formation with NADP+ [7].
实验方案
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
参考文献

[1]Bologna M, Muzi P, et al. Finasteride dose-dependently reduces the proliferation rate of the LnCap human prostatic cancer cell line in vitro. Urology. 1995 Feb;45(2):282-90.

[2]Azzolina B, Ellsworth K, et al. Inhibition of rat alpha-reductases by finasteride: evidence for isozyme differences in the mechanism of inhibition. J Steroid Biochem Mol Biol. 1997 Apr;61(1-2):55-64.

[3]Soni KK, Shin YS, et al. Protective effect of DA-9401 in finasteride-induced apoptosis in rat testis: inositol requiring kinase 1 and c-Jun N-terminal kinase pathway. Drug Des Devel Ther. 2017 Oct 11;11:2969-2979.

[4]Bowman CJ, Barlow NJ, et al. Effects of in utero exposure to finasteride on androgen-dependent reproductive development in the male rat. Toxicol Sci. 2003 Aug;74(2):393-406. Epub 2003 May 28.

[5]Frau R, Mosher LJ, et al. The neurosteroidogenic enzyme 5α-reductase modulates the role of D1 dopamine receptors in rat sensorimotor gating. Psychoneuroendocrinology. 2016 Jan;63:59-67.

[6]Finasteride

[7] Azzolina B. Inhibition of rat alpha-reductases by finasteride: evidence for isozyme differences in the mechanism of inhibition. J Steroid Biochem Mol Biol. 1997 Apr;61(1-2):55-64.

[8]Weisser H. In vitro inhibition of androstenedione 5alpha-reduction by finasteride in epithelium and stroma of human benign prostatic hyperplasia. J Steroid Biochem Mol Biol. 1998 Oct;67(1):49-55. doi: 10.1016/s0960-0760(98)00071-5.

[9]Bologna M. Finasteride dose-dependently reduces the proliferation rate of the LnCap human prostatic cancer cell line in vitro. Urology. 1995 Feb;45(2):282-90.

[10]Wang LG. Down-regulation of prostate-specific antigen expression by finasteride through inhibition of complex formation between androgen receptor and steroid receptor-binding consensus in the promoter of the PSA gene in LNCaP cells. Cancer Res. 1997 Feb 15;57(4):714-9.

[11]Clark RL. External genitalia abnormalities in male rats exposed in utero to finasteride, a 5 alpha-reductase inhibitor. Teratology. 1990 Jul;42(1):91-100.