222989-99-3
中文名称
222989-99-3
英文名称
Finasteride (acetate)
CAS
222989-99-3
分子式
C25H40N2O4
分子量
432.596
MOL 文件
222989-99-3.mol
222989-99-3 结构式
常见问题列表
生物活性
Finasteride (MK-906) acetate 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 acetate 对 II 型 5α-还原酶的亲和力比对 I 型酶高约 100 倍。Finasteride acetate 可用于研究前列腺增生 (BPH) 和雄激素性脱发。靶点
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 [
3
H]testosterone (T) to [
3
H]dihydrotestosterone (DHT) in
P. crustosum
.
Cell Viability Assay
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. |