Dutasteride

属性

溶解性	Soluble in ethanol (44 mg/ml), methanol (64 mg/ml), polyethylene glycol 400 (3 mg/ml), and DMSO (62 mg/ml at 25 °C 117mM). Insoluble in water.
存贮条件	储存温度-20°C

描述

应用	Dutasteride是5α-还原酶抑制剂。
产品介绍	Dutasteride is a 5-α-reductase inhibitor that inhibits the conversion of testosterone into dihydrotestosterone (DHT). Dutasteride inhibits both isoforms of 5-α reductase (5 α-Reductase 1/5aR1 and 5 α-Reductase 2/5aR2) to a similar extent (IC50 6nmol/l and 7 nmol/l, respectively), while finasteride only inhibits Type II. Dutasteride competed for binding the LNCaP cell AR with an IC50 approximately 1.5 μM.
生化机理	IC50 Value: Dutasteride(GG745) is a potent inhibitor of both 5alpha-reductase isozymes. Dutasteride may possess off-target effects on the androgen receptor (AR) due to its structural similarity to DHT. in vitro: Dutasteride inhibited (3)H-T conversion to (3)H-DHT and, as anticipated, inhibited T-induced secretion of PSA and proliferation. However the drug also inhibited DHT-induced PSA secretion and cell proliferation (IC(50) approximately 1 microM). Dutasteride competed for binding the LNCaP cell AR with an IC(50) approximately 1.5 microM. High concentrations of dutasteride (10-50 microM), but not finasteride, in steroid-free medium, resulted in enhanced cell death, possibly by apoptosis [1]. Dutasteride reduces cell viability and cell proliferation in both cell lines tested (androgen-responsive (LNCaP) and androgen-unresponsive (DU145) human prostate cancer (PCa)) [2]. in vivo: GG745 has a terminal half-life of approximately 240 h
别名	度他雄胺;(4aR,4bS,6aS,7S,9aS,9bS,11aR)-N-[2,5-Bis(trifluoromethyl)phenyl]-2,4a,4b,5,6,6a,7,8,9,9a,9b,10,11,11a-tetradecahydro-4a,6a-dimethyl-2-oxo-1H-Indeno[5,4-f]quinoline-7-carboxamide; (5α,17β)-N-[2,5-Bis(trifluoromethyl)phenyl]-3-oxo-4-azaandrost-1-ene-17-carboxamide; Avodart; Avolve; GG 745; GI 198745; Veltride