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CAS No. : 164656-23-9
MCE 国际站:Dutasteride
产品活性:Dutasteride (GG745)是5α 还原酶同工酶 (5α-reductase isozymes) 抑制剂,还可能因其结构域DHT相似对雄激素受体 (AR) 产生脱靶效应。
研究领域:Metabolic Enzyme/Protease | Apoptosis
作用靶点:5 alpha Reductase | Apoptosis
In Vitro: Dutasteride inhibits 3H-T conversion to 3H-DHT and, as anticipated, inhibits T-induced secretion of PSA and proliferation. However the drug also inhibited DHT-induced PSA secretion and cell proliferation (IC50 approximately 1 μM). Dutasteride competes for binding the LNCaP cell AR with an IC50 approximately 1.5 μM. High concentrations of dutasteride (10-50 μM), but not finasteride, in steroid-free medium, resulted in enhanced cell death, possibly by apoptosis. Dutasteride reduces cell viability and cell proliferation in both cell lines tested (androgen-responsive (LNCaP) and androgen-unresponsive (DU145) human prostate cancer (PCa)) .
In Vivo: GG745 has a terminal half-life of approximately 240 hr, and single doses of >10 mg decreased DHT levels significantly more than did single 5-mg doses of finasteride.In placebo treated men without prostate cancer there was an 8.3% median increase in PSA at month 24 compared with -59.5% in those who received dutasteride, using doubled values to correct for dutasteride treatment.Toxicity: Dutasteride may affect male fertility and steroid hormone dynamics. Therefore, a 21-day reproduction study was conducted to determine the effects of dutasteride (10, 32 and 100 μg/L) on fish reproduction. Exposure to dutasteride significantly reduced fecundity of fish and affected several aspects of reproductive endocrine functions in both males and females.
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