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ダルナビル

ダルナビル 化学構造式
206361-99-1
CAS番号.
206361-99-1
化学名:
ダルナビル
别名:
ダルナビル
英語化学名:
Darunavir
英語别名:
D03656;TMC-114;UIC-94017;Darunavir;Darunavir (usan/inn);Darunavir( UIC-94017,TMC-114);Darunaviroxy-1-phenylbutan-2-yl]carbamate;(3R,3AS,6aR)-hexahydrofuro[2,3-b]furan-3-yl ((2S,3R)-4-(4-amino-N-isobutylphenylsulfonamido)-3;(3R,3AS,6aR)-hexahydrofuro[2,3-b]furan-3-yl ((2S,3R)-4-(4-amino-N-isobutylphenylsulfonamido)-3-hydroxy-1-phenylbutan-2-yl)carbamate;(3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl [(2S,3R)-4-{[(4-aminophenyl)sulfonyl](2-methylpropyl)amino}-3-hydroxy-1-phenylbutan-2-yl]carbamate
CBNumber:
CB51176244
化学式:
C27H37N3O7S
分子量:
547.66
MOL File:
206361-99-1.mol

ダルナビル 物理性質

融点 :
74-760C
貯蔵温度 :
-20°C Freezer
外見 :
powder
色:
white to beige

安全性情報

WGK Germany  3

ダルナビル 価格 もっと(6)

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) W01TRCD193500 ダルナビル
Darunavir
206361-99-1 1mg ¥12500 2018-12-26 購入
富士フイルム和光純薬株式会社(wako) W01TRCD193500 ダルナビル
Darunavir
206361-99-1 5mg ¥15000 2018-12-26 購入
Sigma-Aldrich Japan SML0937 ≥98% (HPLC)
Darunavir ≥98% (HPLC)
206361-99-1 10mg ¥19200 2018-12-25 購入
Sigma-Aldrich Japan SML0937 ≥98% (HPLC)
Darunavir ≥98% (HPLC)
206361-99-1 50mg ¥77900 2018-12-25 購入
富士フイルム和光純薬株式会社(wako) W01TRCD193500 ダルナビル
Darunavir
206361-99-1 50mg ¥78800 2018-12-26 購入

ダルナビル 化学特性,用途語,生産方法

化学的特性

White Amorphous Solid

使用

Second generation HIV-1-protease inhibitor; structurally similar to amprenavir. Antiviral

定義

ChEBI: An N,N-disubstituted benzenesulfonamide bearing an unsubstituted amino group at the 4-position, used for the treatment of HIV infection. A second-generation HIV protease inhibitor, darunavir was designed to form robust interactions with the protease enzyme from many strains of HIV, including those from treatment-experienced patients with multiple resistance mutations to other protease inhibitors.

獲得抵抗性

Darunavir is less affected than other protease inhibitors by mutations to resistance, but subgroups with more than 10 cumulative mutations show a >10-fold (median value) decrease in susceptibility. The major resistance mutations occur at positions 50 (150V), 54 (I50M/L), 76 (L76V) and 84 (I84V) of the protease gene.

応用例(製薬)

A synthetic compound formulated as the ethanolate for oral use in combination with ritonavir.

薬物動態学

Oral absorption: c. 82%
Cmax 600 mg once daily + ritonavir 100 mg twice daily: c. 6500 μg/L
Cmin 600 mg oral + ritonavir 100 mg twice daily: c. 3578 μg/L
Plasma half-life: c. 15 h
Volume of distribution: c. 131 L
Plasma protein binding: c. 95%
A single 600 mg dose given orally in combination with ritonavir 100 mg every 12 h increased the systemic exposure of darunavir approximately 14-fold. The relative bioavailability is 30% lower when administered with food in the presence of low-dose ritonavir. Distribution into human CSF, semen or breast milk has not yet been determined.
At least three oxidative metabolites, mediated predominantly through CYP3A4, have been identified in humans; all are at least 10-fold less active than the parent compound against HIV. Around 80% and 14% of the dose is found in the feces and urine, respectively. It should be used with caution in mild–moderate hepatic impairment and avoided in patients with more severe impairment.

臨床応用

Treatment of HIV infection (in combination with other antiretroviral drugs)

副作用

In phase III studies the most common adverse events were diarrhea, nausea, headache and nasopharyngitis. Patients coinfected with hepatitis B or C did not have a higher incidence of adverse events.

ダルナビル 上流と下流の製品情報

原材料

準備製品


ダルナビル 生産企業

Global( 130)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
Alpha Biopharmaceuticals Co., Ltd
0086-411-39042497
0086-411-39042693 sales@alphabiopharm.com China 1954 58
Henan DaKen Chemical CO.,LTD.
+86-371-55531817
info@dakenchem.com CHINA 22043 58
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com CHINA 20786 55
Chemwill Asia Co.,Ltd.
86-21-51086038
86-21-51861608 chemwill_asia@126.com;sales@chemwill.com;chemwill@hotmail.com;chemwill@gmail.com CHINA 24118 58
career henan chemical co
+86-371-86658258
sales@coreychem.com CHINA 19997 58
Hubei widely chemical technology Co., Ltd. 027-83991130
027-83991130 1718093273@QQ.COM China 1026 58
Chembest Research Laboratories Limited +86(0)21-20908456
+86(0)21-58180499 sales@biochembest.com; market@biochembest.com China 6013 61
Beijing Huikang Boyuan Chemical Tech Co., Ltd 010-68862197
010-68882204 bjhkby@126.com China 100 61
Shanghai Boyle Chemical Co., Ltd.
86-21-57758967 sales@boylechem.com China 2928 55
J & K SCIENTIFIC LTD. 400-666-7788 +86-10-82848833
+86-10-82849933 jkinfo@jkchemical.com;market6@jkchemical.com China 96815 76

206361-99-1(ダルナビル)キーワード:


  • 206361-99-1
  • [(1S,2R)-3-[[(4-Aminophenyl)sulfonyl](2-methylpropyl)amino]-2-hydroxy-1-(phenyl-methyl)propyl]carabamic Acid (3R,3aS,6aR)-Hexahydrofuro[2,3-b]-furan-3-yl Ester
  • Darunavir
  • TMC-114
  • UIC-94017
  • [(1S,2R)-3-[[(4-Aminophenyl)sulfonyl](2-methylpropyl)amino]-2-hydroxy-1-(phenyl-methyl)propyl]carabamic Acid (3R,3aS,6aR)-Hexahydrofuro[2,3-β]-furan-3-yl Ester
  • [(3R,3aS,6aR)-2,3,3a,4,5,6a-Hexahydrofuro[5,4-b]furan-3-yl] N-[(2S,3R)-4-[(4-aminophenyl)sulfonyl-(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]carbamate
  • Darunavir( UIC-94017,TMC-114)
  • (3R,3AS,6aR)-hexahydrofuro[2,3-b]furan-3-yl ((2S,3R)-4-(4-amino-N-isobutylphenylsulfonamido)-3-hydroxy-1-phenylbutan-2-yl)carbamate
  • (3R,3AS,6aR)-hexahydrofuro[2,3-b]furan-3-yl ((2S,3R)-4-(4-amino-N-isobutylphenylsulfonamido)-3
  • Darunaviroxy-1-phenylbutan-2-yl]carbamate
  • D03656
  • Darunavir (usan/inn)
  • (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl [(2S,3R)-4-{[(4-aminophenyl)sulfonyl](2-methylpropyl)amino}-3-hydroxy-1-phenylbutan-2-yl]carbamate
  • ダルナビル
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