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/ Dutasteride/度他雄胺

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

货号：A190042 同义名： GG 745; GI 198745

Dutasteride是一种强效的双重5α-还原酶同工酶抑制剂。由于其结构与双氢睾酮（DHT）的相似性，Dutasteride可能对**雄激素受体（AR）**产生非靶向效应。

Dutasteride/度他雄胺 化学结构 CAS号：164656-23-9
Dutasteride/度他雄胺 化学结构
CAS号：164656-23-9
Dutasteride/度他雄胺 3D分子结构
CAS号：164656-23-9
Dutasteride/度他雄胺 化学结构 CAS号：164656-23-9
Dutasteride/度他雄胺 3D分子结构 CAS号：164656-23-9
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Dutasteride/度他雄胺 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]}
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全球学术期刊中引用的产品

• Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]
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• Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]
• Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]
• Nat. Nanotechnol., 2025. Ambeed. [ A243018 , A1216705 , A522597 , A125401 , A1355641 ]
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产品名称 5-alpha Reductase ↓ 其他靶点 纯度
Dutasteride ✔ 99%
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/度他雄胺 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/度他雄胺 细胞实验

Cell Line
Concentration Treated Time Description References
human primary alveolar epithelial cells 5 μM 72 h significantly reduced ACE2 levels Cell Stem Cell. 2020 Dec 3;27(6):876-889.e12.
hESC-derived cardiac cells 1 μM, 2 μM, 5 μM 24 h inhibited ACE2 and TMPRSS2 expression Cell Stem Cell. 2020 Dec 3;27(6):876-889.e12.
SH-SY5Y cells 1 µM 24 h To evaluate mitochondrial function parameters. Dutasteride had inconclusive effects on mitochondrial function in SH-SY5Y cells, while finasteride was ineffective. Front Pharmacol. 2022 Jul 22;13:898067.
THP-1 cells 1 µM 24 h To measure the production of proinflammatory markers such as nitric oxide (NO), IL-1β, and IL-6. Dutasteride completely prevented the MPP+-induced increase in these markers, while finasteride was ineffective. Front Pharmacol. 2022 Jul 22;13:898067.
THP1-XBlue cells 1 µM 24 h To evaluate the inhibition of NF-κB inflammatory response. Dutasteride completely prevented the MPP+-induced increase in NF-κB response, while finasteride was ineffective. Front Pharmacol. 2022 Jul 22;13:898067.
human bronchial epithelial cells 5 μM 72 h significantly reduced ACE2 and TMPRSS2 levels Cell Stem Cell. 2020 Dec 3;27(6):876-889.e12.
GT1-7 mouse GnRH neuronal cells 5 μM 24 h To examine the effect of Dutasteride on Gnrh and Kiss1 expression, revealing that Dutasteride inhibits Gnrh and Kiss1 expression BMC Biol. 2022 Jan 7;20(1):11.

Dutasteride/度他雄胺 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6 male mice MPTP-induced Parkinson's disease model Intraperitoneal injection 5 mg/kg and 12.5 mg/kg Once daily for 10 days To evaluate the protective effect of dutasteride on MPTP-induced enteric neuronal damage. Dutasteride at 5 mg/kg completely prevented MPTP-induced damage to dopamine and VIP neurons and inhibited the increase in proinflammatory macrophages. Front Pharmacol. 2022 Jul 22;13:898067.
BALB/c strain of athymic SCID mice LNCaP xenograft tumor model Subcutaneous injection 1 mg/kg Daily administration for 4 days (off-cycle) Dutasteride inhibited initial testosterone-induced tumor regrowth during both the first and second off-cycle and significantly increased survival. J Urol. 2015 Apr;193(4):1388-93
Mice Hsd17b3 KO mice Dietary administration 1.8 mg/kg Daily administration for 30 days To investigate the contribution of SRD5A and the alternate pathway of androgen biosynthesis in maintaining androgen activity in adult Hsd17b3 KO mice. Results showed that dutasteride significantly reduced seminal vesicle weight but did not alter anogenital distance,, testis, or epididymis weights. Additionally, dutasteride decreased serum levels of 5α-DHP and androsterone in Hsd17b3 KO mice, indicating that SRD5A inhibition can reduce androgen biosynthesis via the alternate pathway. FASEB J. 2024 Nov 30;38(22):e70177
SKG mice Curdlan-induced spondyloarthritis model Dietary administration 41.2 mg/kg Started at 9 weeks after the first curdlan injection, continued until 17 weeks Dutasteride increased spinal mineralization, positively correlated with serum IL-17A levels, and decreased serum SOST levels Arthritis Res Ther. 2020 May 24;22(1):121
Mice DSS-induced colitis model Oral 13 μg/g Daily, until puberty onset To examine the effect of Dutasteride on puberty onset, revealing that Dutasteride delays puberty onset BMC Biol. 2022 Jan 7;20(1):11.

Dutasteride/度他雄胺 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/度他雄胺 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/度他雄胺 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/度他雄胺 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/度他雄胺 技术信息

CAS号164656-23-9
分子式C27H30F6N2O2
分子量 528.53
SMILES Code O=C([C@H]1CC[C@]2([H])[C@]1(C)CC[C@]3([H])[C@@]4(C)C=CC(N[C@]4([H])CC[C@]32[H])=O)NC5=CC(C(F)(F)F)=CC=C5C(F)(F)F
MDL No. MFCD00937869
别名 GG 745; GI 198745; LS-173584
运输蓝冰
InChI Key JWJOTENAMICLJG-QWBYCMEYSA-N
Pubchem ID 6918296
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, store in freezer, under -20°C
溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一

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

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