222989-99-3
中文名稱
222989-99-3
英文名稱
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 結(jié)構(gòu)式
常見問題列表
生物活性
Finasteride (MK-906) acetate 是一種有效的競(jìng)爭(zhēng)性 5α-還原酶 (5α-reductase) 抑制劑，對(duì) II 型 5α-還原酶的 IC50 值為 4.2 nM。Finasteride acetate 對(duì) II 型 5α-還原酶的親和力比對(duì) I 型酶高約 100 倍。Finasteride acetate 可用于研究前列腺增生 (BPH) 和雄激素性脫發(fā)。靶點(diǎn)
IC50: 4.2 nM (type II 5α-reductase)
體外研究
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. |
體內(nèi)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. |