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 可用于良性前列腺增生症 (BPH) 和雄激素性脱发的研究。
产品描述
Finasteride (MK-906) acetate is a potent and competitive 5α-reductase inhibitor, with an IC 50 of 4.2 nM for type II 5α-reductase. The affinity of Finasteride acetate for type II 5α-reductase enzyme was approximately 100-fold higher than that for the type I enzyme. Finasteride acetate can be used for the research of benign prostatic hyperplasia (BPH) and androgenic alopecia [1] [2] [3].
体外活性
Finasteride (10 μM; 6-24 h) induces the expression of HO-1 and Nrf2 proteins in PC-3 cells [2]. Finasteride can reduce the conversion of [ 3 H]testosterone (T) to [ 3 H]dihydrotestosterone (DHT) in P. crustosum [1]. Cell Viability Assay [2] 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.
体内活性
Finasteride (0.1-0.5 mg/kg; p.o. once daily for 16 weeks) reduces prostatic size in dogs with BPH while not adversely affecting semen quality or serum testosterone concentration [3]. Animal Model: Male dogs with spontaneous BPH (2.7-11 years old; 10.3-49 kg) [3] 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.
Cas No.
222989-99-3
分子式
C25H40N2O4
分子量
432.6
别名
Finasteride acetate
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years