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.
IC50&Target
IC50: 4.2 nM (type II 5α-reductase)
体外研究
Finasteride (10 μM; 6-24 h) induces the expression of HO-1 and Nrf2 proteins in PC-3 cells.
Finasteride decreases the conversion of [H]testosterone (T) to [H]dihydrotestosterone (DHT) in P. crustosum.
Western Blot Analysis
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
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.
Animal Model:
Male dogs with spontaneous BPH (2.7-11 years old; 10.3-49 kg)
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.
分子式
C23H36N2O2
分子量
372.54
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 : 100 mg/mL (268.43 mM; ultrasonic and warming and heat to 60°C)