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5-alpha还原酶
5 Alpha Reductase 其他类固醇
/ Dutasteride

度他雄胺 /Dutasteride {[allProObj[0].p_purity_real_show]}

货号：A190042 同义名： GG 745;GI 198745

Dutasteride is a potent inhibitor of both 5 alpha-reductase isozymes. Dutasteride may possess off-target effects on the androgen receptor (AR) due to its structural similarity to DHT.

Dutasteride 化学结构 CAS号：164656-23-9
Dutasteride 化学结构
CAS号：164656-23-9
Dutasteride 3D分子结构
CAS号：164656-23-9
Dutasteride 化学结构 CAS号：164656-23-9
Dutasteride 3D分子结构 CAS号：164656-23-9
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Dutasteride 纯度/质量文件 产品仅供科研

货号：A190042 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 5-alpha Reductase ↓ 其他靶点 纯度
Dutasteride ✔ 98%
Finasteride +++

5-α reductase, Ki: 10.2 nM

 		98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Dutasteride 生物活性

靶点

  • 5-alpha Reductase
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]

Dutasteride 动物研究

Dose Mice: 5 mg/kg, 12.5 mg/kg[4] (i.p., SID)
Administration i.p.
Pharmacokinetics
Animal Rats[5]
Dose 2.5 mg/kg (i.v.)
5 mg/kg (p.o.)
Administration i.v.
p.o.
AUCinf 1148 ± 81 μg·min/ml (i.v.)
T1/2 1607 ± 196 min (i.v.)
Tmax 60 min (p.o.)
AUClast 275 ± 9 μg·min/ml (p.o.)
CL 2.19 ± 0.16 ml/min/kg (i.v.)
Cmax 289 ± 10 ng/ml (p.o.)
Vss 4900 ± 326 ml/kg (i.v.)

Dutasteride 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 <<

Dutasteride 参考文献

[1]Jun JEJ, Kinkade A, et al. 5α-Reductase Inhibitors for Treatment of Benign Prostatic Hyperplasia: A Systematic Review and Meta-Analysis. Can J Hosp Pharm. 2017;70(2):113-119.

[2]Frye SV. Discovery and clinical development of dutasteride, a potent dual 5alpha-reductase inhibitor. Curr Top Med Chem. 2006;6(5):405-21.

[3]Vitalis OO, Christopher CO. The Role of Dutasteride in Acute Prostatic Haematuria. 2017 Nov Vol.8 No.11.

[4]Litim N, Bourque M, et al. The 5α-reductase inhibitor Dutasteride but not Finasteride protects dopamine neurons in the MPTP mouse model of Parkinson's disease. Neuropharmacology. 2015 Oct;97:86-94.

[5]Seo SW, Park JW, et al. In Vitro and In Vivo Assessment of Metabolic Drug Interaction Potential of Dutasteride with Ketoconazole. Pharmaceutics. 2019 Dec 11;11(12). pii: E673.

Dutasteride 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.89mL

0.38mL

0.19mL

9.46mL

1.89mL

0.95mL

18.92mL

3.78mL

1.89mL

Dutasteride 技术信息

CAS号164656-23-9
分子式C27H30F6N2O2
分子量 528.53
别名 GG 745;GI 198745;LS-173584
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,Store in freezer, under -20°C
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
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

Tags: Dutasteride | GG 745;GI 198745;LS-173584 | Other Steroids | 5-alpha Reductase | AmBeed-信号通路专用抑制剂 | Dutasteride 纯度/质量文件 | Dutasteride 亚型比较 | Dutasteride 生物活性 | Dutasteride 动物研究 | Dutasteride 临床数据 | Dutasteride 参考文献 | Dutasteride 实验方案 | Dutasteride 技术信息

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