产品说明书
Dutasteride
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同义名 : | GG 745;GI 198745;LS-173584 |
| CAS号 : | 164656-23-9 | |
| 货号 : | A190042 | |
| 分子式 : | C27H30F6N2O2 | |
| 纯度 : | 98% | |
| 分子量 : | 528.53 | |
| MDL号 : | MFCD00937869 | |
| 存储条件： |
粉末 Sealed in dry,Store in freezer, under -20°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 35 mg/mL(66.22 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
IP 2% DMSO+2% Tween80+30% PEG300+water 2 mg/mL clear PO 0.5% CMC-Na 50 mg/mL suspension |
| 生物活性 | |||
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| 靶点 |
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| 描述 | 5 alpha Reductases (5ARs) are important enzymes for the progression of benign prostatic hyperplasia by converting testosterone to dihydrotestosterone with 2 isoenzymes. Dutasteride is a competitive inhibitor of 5ARs with IC50 value of 6 nM for type-1 5-AR and 7 nM for type-2 5-AR. In a study, 1879 BPH patients were treated with 0.5 mg dutasteride daily or combined treated with other drugs like tamsulosin and alfuzosin. The results found that IPSS score point was meanly reduced about 6.5-point. The adverse events in the dutasteride group was not statistically significant with OR 1.10.[1] Dutasteride is 60-fold more potential towards type 1 5AR and also is most potent dual 5AR inhibitor. In a male rats model of prostate growth, daily treated them with dutasteride at 1, 10, or 100 mg/kg found no significant difference between these dose groups, indicating that a stronger potent when the maximum effect in this model achieved at 1 mg/kg/day. In the rats model, the half-life, total body clearance, volume at steady-state and oral bioavailability of 1 mg/kg/day dutasteride were 13.7 hr, 4.1 mL/min/kg, 4 L/kg and 100% respectively. While in dog model with oral administration of 5 mg/kg dutasteride, these values were 65 hr, 0.5 mL/min/kg, 3L/kg and 43% respectively. Dutasteride doses of 0.01 to 40 mg were studied iin some Phase I studies, the results showed that the absolute bioavailability ranged from 40-100% as well as production of a dose related decrease in DHT. No effect when single oral doses < 0.1 mg while significantly decreasing of DHT when oral dutasteride doses > 5 mg. The peak decreasing was 95% at concentration of 40 mg. Furthermore, dutasteride doses of 0.1, 0.5, 2.5, 2.5 and 5 mg were studied in 53 BPH patients, >=95% decreasing of DHT was observed at doses of 2.5mg/day and up.[2] | ||
| 作用机制 | Dutasteride-5α reductase is a stable complex with a slow dissociation rate, thereby preventing the enzymes from binding to testosterone.[3] | ||
| 临床研究 | |||||
|---|---|---|---|---|---|
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT02147964 | Gonadotropin Deficiency | Phase 2 | Not yet recruiting | December 2026 | United States, Washington ... 展开 >> University of Washington Medical Center (Health Sciences) Not yet recruiting Seattle, Washington, United States, 98195 Contact: Iris Nielsen 206-221-5473 nielseni@uw.edu Contact: Kathy Winter 206-616-0484 klwinter@uw.edu Principal Investigator: Mara Roth, MD Sub-Investigator: John Amory, MD, MPH Sub-Investigator: Stephanie Page, MD, PhD Sub-Investigator: Bradley Anawalt, MD 收起 << |
| NCT00298155 | - | Completed | - | - | |
| NCT00298155 | Cancer Prosta... 展开 >>te Neoplasms 收起 << | Phase 2 | Completed | - | United States, Washington ... 展开 >> Veterans' Administration Puget Sound Health Care System (VAPSHCS) Seattle, Washington, United States, 98108-1532 University of Washington Seattle, Washington, United States, 98195-6158 收起 << |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
1.89mL 0.38mL 0.19mL |
9.46mL 1.89mL 0.95mL |
18.92mL 3.78mL 1.89mL |
| 参考文献 |
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