基本信息

产品描述

Dutasteride是5α-还原酶抑制剂。

靶点（IC50 & Targe）

5-α reductase

体外研究

Dutasteride抑制Ⅰ型5AR和Ⅱ型5AR，其IC50分别为6 nM和Dutasteride对Ⅰ型5AR的抑制作用是Finasteride的60倍，使酶失活的速度是Finasteride的～5倍。[1] Dutasteride抑制(3)H-T转化为(3)H-DHT，并且如预期的，抑制LNCaP细胞中T诱导的PSA分泌和增殖。Dutasteride也会抑制LNCaP 细胞中DHT诱导的PSA分泌和细胞增殖，其IC50为1 μM。Dutasteride竞争性结合LNCaP细胞的AR，IC50 值为1.5 μM。Dutasteride (10–50 μM)在无类固醇的培养基中增加了细胞死亡，可能由细胞凋亡引起。[2] Dutasteride降低了雄性激素响应(LNCaP)的和雄性激素不响应(DU145)的人类前列腺癌(PCa)细胞系的细胞活性和增殖。在雄性激素响应(LNCaP)的细胞中，Dutasteride导致参与雄性激素(HSD17B1;HSD17B3;CYP11B2) 的生物合成和代谢的蛋白编码基因，雄激素受体和雄激素受体共调节因子（AR; CCND1）以及信号转导（ERBB2;V-CAM; SOS1 ）基因的过表达，然而，减少表达的基因(KLK3; KLK2; DHCR24)为雄性激素调节因子基因(ARGs)。[3] Dutasteride抑制前列腺癌细胞中FASN mRNA，蛋白质表达和酶活性。[4]

体内研究

Dutasteride (100毫克/千克/天)处理的完好雄性大鼠，与仅用载体处理的相比，前列腺仅有其一半大。Dutasteride口服生物有效，且由于其作用机制，它能容易地克服>99%血浆蛋白结合的潜在不利因素。[1]

参考文献

[1] Frye SV, et al. Curr Top Med Chem, 2006, 6(5), 405-421.

[2] Lazier CB, et al. Prostate, 2004, 58(2), 130-144.

[3] Biancolella M, et al. Invest New Drugs, 2007, 25(5), 491-497.

[4] Schmidt LJ, et al. Prostate, 2007, 67(10), 1111-1120.

安全信息

图形或危害标志
提示语	Warning
危险说明	H302 H410
防范说明	P264 P270 P273 P301+P312 P330 P391 P501
UN号码	3077
危险分类	9
包装等级	III

基本信息

安全信息

图形或危害标志
危险性说明	H315: Causes skin irritation. H319: Causes serious eye irritation. H335: May cause respiratory irritation.
防范说明	P233: Keep container tightly closed. P260: Do not breathe . P261: Avoid breathing . P264: Wash hands thoroughly after handling. P271: Use only outdoors or in a well-ventilated area. P280: Wear . P302 + P352: IF ON SKIN: Wash with plenty of soap and water. P304: IF INHALED: Remove victim to fresh air and keep at rest in a position comfortable for breathing.. P304 + P340: IF INHALED: Remove victim to fresh air and keep at rest in a position comfortable for breathing. P305 + P351 + P338: IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continue rinsing. P312: Call a POISON CENTER or doctor/physician if you feel unwell. P321: Specific treatment (see relevant procedures. on this label). P332 + P313: If skin irritation occurs: Get medical advice/ attention. P337 + P313: If eye irritation persists: Get medical advice/attention. P340: Remove victim to fresh air and keep at rest in a position comfortable for breathing. P362: Take off contaminated clothing and wash before reuse. P403: Store in a well-ventilated place. P403 + P233: Store in a well-ventilated place. Keep container tightly closed. P405: Store locked up. P501: Dispose of contents/container to in accordance with local regulation .