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ズタステリド

ズタステリド 化学構造式
164656-23-9
CAS番号.
164656-23-9
化学名:
ズタステリド
别名:
ズタステリド;デュタステリド;デュタステリド (JAN)
英語化学名:
Dutasteride
英語别名:
Avolve;Duagen;Avodart;(5α,17β)-;GI 198745;DUTASTERIDE;Dutasteride API;Dutasteride CRS;GG-745, GI-198745,;5,6-Dehydro-17&beta
CBNumber:
CB3254628
化学式:
C27H30F6N2O2
分子量:
528.53
MOL File:
164656-23-9.mol

ズタステリド 物理性質

融点 :
242-250°C
沸点 :
620.3±55.0 °C(Predicted)
比重(密度) :
1.303±0.06 g/cm3(Predicted)
貯蔵温度 :
-20°C
溶解性:
DMSO: soluble2mg/mL, clear
酸解離定数(Pka):
13.32±0.70(Predicted)
外見 :
powder
色:
white to beige
光学活性 (optical activity):
[α]/D +18 to +24°, c = 1 in chloroform-d
InChIKey:
JWJOTENAMICLJG-QWBYCMEYSA-N

安全性情報

HSコード  2937290000

ズタステリド 価格 もっと(18)

メーカー 製品番号 製品説明 CAS番号 包装 価格 更新時間 購入
富士フイルム和光純薬株式会社(wako) W01FLC079399 ズタステリド
Dutasteride
164656-23-9 250mg ¥71300 2021-03-23 購入
富士フイルム和光純薬株式会社(wako) W01FLC079399 ズタステリド
Dutasteride
164656-23-9 1g ¥177500 2021-03-23 購入
富士フイルム和光純薬株式会社(wako) W01MAS076047
Dutasteride
164656-23-9 5g ¥351700 2021-03-23 購入
Sigma-Aldrich Japan 1229922 United States Pharmacopeia (USP) Reference Standard
Dutasteride United States Pharmacopeia (USP) Reference Standard
164656-23-9 200mg ¥103000 2021-03-23 購入
Sigma-Aldrich Japan SML1221 ≥98% (HPLC)
Dutasteride ≥98% (HPLC)
164656-23-9 10mg ¥17400 2021-03-23 購入

ズタステリド 化学特性,用途語,生産方法

用途

デュタステリド(Dutasteride)は、テストステロンからのジヒドロテストステロン(DHT)生成を阻害する5α-還元酵素トリプル阻害薬(英語版)である。前立腺肥大症および男性型脱毛症の治療に用いられる。

効能

前立腺肥大症治療薬, 抗アンドロゲン薬, 5α還元酵素阻害薬

商品名

アボルブ (グラクソ・スミスクライン); ザガーロ (グラクソ・スミスクライン)

説明

Dutasteride was launched for the symptomatic treatment of benign prostatic hyperplasia. Dutasteride can be prepared from 3-oxo-4-androstene-17β-carboxylic acid by several ways in 6 or 8 steps. Dutasteride is a dual inhibitor of type 1 and 2 isoforms of 5α-reductase unlike finasteride, the first marketed 5α-reductase inhibitor, which only acts on type 2 isozyme. Dutasteride is a 3-fold greater inhibitor of type-2 5α-reductase than finasteride in men and has greater effect on the type-l than on type-2 isozyme. In animal models,dutasteride exhibited superior efficacy and pharmacokinetics compared to finasteride. In patients with benign prostate hyperplasia, administration of dutasteride was shown to dose-dependently decrease serum dihydrotestosterone levels with greater efficacy as compared to finasteride (95% vs 67%). Serum testosterone levels increased with both active drugs, in conjunction with dihydrotestosterone suppression but remained within normal ranges. In long term studies, in men with moderate to severe benign prostate hyperplasia, once daily dutasteride significantly reduced prostate volume, reduced the risk of acute urinary retention and surgery by 57% and improved lower urinary tract symptoms and urinary flow measurements. After oral administration, dutasteride is rapidly absorbed, has a short distribution phase and a mean bioavailability of 60%. The high volume of distribution, combined with its low linear clearance results in a prolonged dose dependent half-life (from 3 days at low concentrations to 5 weeks at high concentrations) whereas finasteride’s half-life time is approximately 10 h. Dutasteride is well tolerated and the most occurring adverse events are impotence, decrease in libido, ejaculation disorders and gynaecomastia. Unlike a-blockers which primarily act acutely on benign prostatic hyperplasia symptoms, 5a-reductase inhibitors can alter disease progression. Concomitant administration of dutasteride did not affect the pharmacokinetics of either tamsulosin or terazosin. In addition, the tolerability of both terazosin and tamsulosin were improved during combination therapy.

化学的特性

White Crystalline Solid

Originator

GlaxoSmithKline (UK)

使用

Used in the treatment of benign prostatic hyperplasia. Dual inhibitor of 5a-reductase isoenzymes type 1 and 2; structurally related to Finasteride.

使用

Used in the treatment of benign prostatic hyperplasia. Dual inhibitor of 5α-reductase isoenzymes type 1 and 2; structurally related to Finasteride.

使用

antihypertensive, ACE inhiibitor

使用

Dutasteride is a dual inhibitor of 5α-reductase isoenzymes type 1 and 2; structurally related to Finasteride (F342000). Dutasteride is used in the treatment of benign prostatic hyperplasia.

定義

ChEBI: Finasteride in which the tert-butyl group is replaced by a 2,5-bis(trifluoromethyl)phenyl group. A synthetic 4-azasteroid, dutasteride is a selective inhibitor of both the type 1 and type 2 isoforms of steroid 5alpha-reductase an intracellular enzyme that converts testosterone to 5alpha-dihydrotestosterone. Dutasteride is used for the treatment of symptomatic benign prostatic hyperplasia in men with an enlarged prostate gland.

brand name

Avodart (GlaxoSmithKline).

生物学の機能

Similar to finasteride, dutasteride is a competitive and mechanism-based inhibitor not only of type 2 but also of type 1 5α-reductase isoenzymes, with which stable enzyme-NADP adduct complexes are formed, inhibiting the conversion of testosterone to DHT. The suppression of both type 1 and type 2 isoforms results in greater and more consistent reduction of plasma DHT than that observed for finasteride. The more effective dual inhibition of type 1 and type 2 5α-reductase isoforms lowers circulating DHT to a greater extent than with finasteride and shows advantages in treating BPH and other disease states (e.g., prostate cancer) that are DHT-dependent.

薬物動態学

The maximum effect of 0.5 mg daily doses of dutasteride on the suppression of DHT is dose-dependent and is observed within 1 to 2 weeks. After 2 weeks of 0.5 mg daily dosing, median plasma DHT concentrations were reduced by 90%, and after 1 year, the median decrease in plasma DHT was 94%. The median increase in plasma testosterone was 19% but remained within the physiological range. The drug also reduced serum prostatic specific antigen by approximately 50% at 6 months and total prostate volume by 25% at 2 years. Dutasteride produced improvements in quality of life and peak urinary flow rate and reduction of acute urinary retention without the need for surgery.

副作用

The main side effects are ED, decreased libido, gynecomastia, and ejaculation disorders. Long-term use (>4 years), however, did not reveal increased onset of sexual side effects. In addition, the combination of dutasteride and tamsulosin is well-tolerated and has the added advantage of rapid symptomatic relief.

ズタステリド 上流と下流の製品情報

原材料

準備製品


ズタステリド 生産企業

Global( 360)Suppliers
名前 電話番号 ファックス番号 電子メール 国籍 製品カタログ 優位度
Shanghai Biolang Biotechnology Co., Ltd.
+8613669031409
+8613669031409 Jason@biolang.cn China 1229 58
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com CHINA 22607 55
Guangzhou PI PI Biotech Inc
+8618371201331
020-81716319 sales@pipitech.com;87478684@qq.com China 3245 55
Shanghai Yingrui Biopharma Co., Ltd.
+86-21-33585366 E-mail:sales03@shyrchem.com
+86-21-34979012 sales03@shyrchem.com CHINA 739 60
Hubei XinRunde Chemical Co., Ltd.
+8615102730682
02783214688 bruce@xrdchem.cn CHINA 567 55
Nanjing Finetech Chemical Co., Ltd.
025-85710122 17714198479
025-85710122 sales@fine-chemtech.com CHINA 890 55
ATK CHEMICAL COMPANY LIMITED
+86 21 5161 9050/ 5187 7795
+86 21 5161 9052/ 5187 7796 ivan@atkchemical.com CHINA 26734 60
Hefei TNJ Chemical Industry Co.,Ltd.
86-0551-65418684 18949823763
86-0551-65418684 info@tnjchem.com China 3001 55
career henan chemical co
+86-371-86658258
sales@coreychem.com CHINA 29959 58
Shaanxi Yikanglong Biotechnology Co., Ltd.
17791478691
yklbiotech@163.com CHINA 297 58

164656-23-9(ズタステリド)キーワード:


  • 164656-23-9
  • (1S,2R,7R,10S,11S,14S,15S)-N-[2,5-bis(trifluoroMethyl)phenyl]-2,15-diMethyl-5-oxo-6-azatetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadec-3-ene-14-carboxaMide
  • (4aR,4bS,6aS,7S,9aS,9bS,11aR)-N-[2,5-Bis(trifluoroMethyl)phenyl]-2,4a,4b,5,6,6a,7,8,9,9a,9b,10,11,11a-tetradecahydro-4a,6a-diMethyl-2-oxo-1H-Indeno[5,4-f]quinoline-7-carboxaMide
  • (5α,17β)-
  • (4aR,4bS,6aS,7S,9aS,9bS,11aR)-N-[2,5-Bis(trifluoroMethyl)phenyl]-2,4a,4b,5,6,6a,7,8,9,9a,9b,10,11,11a-tetradecahydro-4a,6a-diMethyl-2-oxo-1H-indeno[5,4-f]quinoline-7-carboxaMide-13C6
  • 6β-Hydroxy Dutasteride
  • 4-Azaandrost-1-ene-17-carboxaMide, N-[2,5-bis(trifluoroMethyl)phenyl]-3-oxo-, (5a,17b)-
  • Avolve
  • 5,6-Dehydro-17&alpha
  • Dutasteride API
  • (4aR,4bS,6aS,7S,9aS,9bS,11aR)-N-(2,5-Bis(trifluoroMethyl)phenyl)-4a,6a-diMethyl-2-oxo-2,4a,4b,5,6,6a,7,8,9,9a,9b,10,11,11a-tetradecahydro-1H-indeno[5,4-f]quinoline-7-carboxaMide
  • Dutasteride for system suitability
  • Dutasteride (200 mg)
  • Duagen
  • (5a,17)-N-[2,5-Bis(trifluoromethyl)phenyl]-3-oxo-4-azaandrost-1-ene-17-carboxamide
  • Avodart
  • GI 198745
  • GG-745, GI-198745,
  • 5α,17β)-N-[2,5-Bis(trifluoromethyl)phenyl]-3-oxo-4- Aza -androst-1-ene-17-carboxamide
  • (5alpha,17beta)-n-{2,5-bis(trifluoromethyl)phenyl}-3-oxo-4-azaandrost-l-ene-17-carboxamide
  • DUTASTERIDE
  • Dutasteride(Avodart)
  • Dutasteride (GG-745)
  • 5,6-Dehydro-17&beta
  • Dutasteride CRS
  • Dutasteride for system suitability CRS
  • 1H-Indeno[5,4-f]quinoline-7-carboxamide, N-[2,5-bis(trifluoromethyl)phenyl]-2,4a,4b,5,6,6a,7,8,9,9a,9b,10,11,11a-tetradecahydro-4a,6a-dimethyl-2-oxo-, (4aR,4bS,6aS,7S,9aS,9bS,11aR)-
  • Dutasteride USP/EP/BP
  • Dutasteride (1.0mg/ml in DMSO)
  • ズタステリド
  • デュタステリド
  • デュタステリド (JAN)
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