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オセルタミビル

 オセルタミビル 化学構造式
196618-13-0
CAS番号.
196618-13-0
化学名:
オセルタミビル
别名:
オセルタミビル
英語化学名:
OSELTAMIVIR
英語别名:
TaMvir;TAMIFLU;GS 4104;GOP-A-Flu;OSELTAMIVIR;OSTELTAMIVIR;TaMiflu-Free;Oseltamivir (free base);(3R,5S)-ethyl 4-acetamido-5-amino-3-(pentan-3-yloxy)cyclohex-1-enecarboxylate;(3R,4R,5S)-Ethyl 4-acetamido-5-amino-3-(pentan-3-yloxy)cyclohex-1-enecarboxylate
CBNumber:
CB1472402
化学式:
C16H28N2O4
分子量:
312.4
MOL File:
196618-13-0.mol

オセルタミビル 物理性質

酸解離定数(Pka):
7.7 (25°); 6.6 (70°)
CAS データベース:
196618-13-0

安全性情報

オセルタミビル 価格

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

オセルタミビル 化学特性,用途語,生産方法

効能

抗ウイルス薬, ノイラミニダーゼ阻害薬

定義

ChEBI: A cyclohexenecarboxylate ester that is the ethyl ester of oseltamivir acid. An antiviral prodrug (it is hydrolysed to the active free carboxylic acid in the liver), it is used to slow the spread of influenza.

抗菌性

Oseltamivir is active against influenza A and B, but no other virus.

獲得抵抗性

Mutations in the neuraminidase (H274Y) have been detected in treated patients with seasonal H1N1 infection. Cross-resistance with zanamivir has been described in vitro.

応用例(製薬)

A selective neuraminidase inhibitor, formulated as the phosphate salt of the ethyl ester for oral administration.

薬物動態学

Oral absorption: c. 75%
Cmax 75 mg oral: 0.35–0.55 mg/L after 4 h
Plasma half-life: 7–9 h
Plasma protein binding: Not known
The ethyl ester prodrug is hydrolyzed by hepatic esterases to release the active compound, oseltamivir carboxylate. Drug is excreted in the urine as the carboxylate derivative.

臨床応用

Treatment and prevention of susceptible influenza A (H3N2) and B infections in adults and young children

副作用

Adverse events relate to the gastrointestinal tract; the most common is nausea with or without vomiting in 10% of patients. Food alleviates side effects.

酵素阻害剤

This zanamivir analogue (FW = 284.36 g/mol), also known by its code name GS 4071, and systematic name (3R,4R,5S) -5-amino-4-acetamido-3- (pentan-3-yloxy) cyclohex-1-ene-1-carboxylate, is a potent inhibitor of influenza A and B neuraminidase (IC50 = 1 nM). The pro-drug ester (FW = 312.40 g/mol; CAS 196618-13-0; Generic Name: Oseltamivir; Systematic Name: ethyl (3R,4R,5S) -5-amino-4-acetamido-3- (pentan-3-yloxy) - cyclohex-1-ene-1-carboxylate; tradename: Tamiflu®) is known as oseltamivir. Pharmacokinetics: Oseltamivir is readily absorbed from the gastrointestinal tract and is subsequently converted by hepatic esterases to its pharmacologically active form (oseltamivir carboxylate). It is widely distributed in the body, showing a half-life is 6 to 10 hours. The drug is excreted primarily through the kidneys, and dosing must be adjusted for patients with renal insufficiency. Oseltamivir achieves high plasma levels and thus can be effective beyond the respiratory tract. (See Zanamivir) Potential Use as an Antipandemic Agent: Analysis data for patients (all ages) admitted to hospital worldwide with laboratory-confirmed or clinically diagnosed infection with the pandemic influenza A H1N1pdm09 virus indicates that early treatment in adults admitted to hospital with suspected/proven influenza infection can be effective in reducing mortality . In the United States, tamiflu has been stockpiled as the front line of its national pandemic defense strategy. Indeed oseltamivir’s producer, Roche, in coordination with external partners now possesses the capacity to produce more than 400 million courses of Tamiflu yearly.

オセルタミビル 上流と下流の製品情報

原材料

準備製品


オセルタミビル 生産企業

Global( 84)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
Beijing Cooperate Pharmaceutical Co.,Ltd.
+86-10-60279497 +86(0)15646567669
+86-10-60279497 sales01@cooperate-pharm.com CHINA 1530 55
ATK CHEMICAL COMPANY LIMITED
+86 21 5161 9050/ 5187 7795
+86 21 5161 9052/ 5187 7796 ivan@atkchemical.com CHINA 24196 60
Nanjing Dolon Biotechnology Co.,Ltd.
18905173768
sales@dolonchem.com CHINA 2972 58
Hubei Jusheng Technology Co.,Ltd.
86-188-71490254
peter@hubeijusheng.com CHINA 20095 58
Casorganics US Corp
+17326109938
sales@casorganics.com CHINA 141 58
3B Pharmachem (Wuhan) International Co.,Ltd. 86-21-50328103 * 801、802、803、804 Mobile:18930552037
86-21-50328109 3bsc@sina.com China 15884 69
JinYan Chemicals(ShangHai) Co.,Ltd. 13817811078,021-50426030
86-021-50426522,50426273 sales@jingyan-chemical.com China 10012 60
Jia Xing Isenchem Co.,Ltd 0573-85280080,18627885956
0573-85285100 isenchem@163.com,QQ:2446116053 China 9744 66
Chemfun Medical Technology(Shanghai) Co., Ltd. 021-67220633 & 021-37212706
+86-21-67220638 chemfun@chemfun.net China 21815 59
LGM Pharma 1-(800)-881-8210
615-250-9817 inquiries@lgmpharma.com United States 1943 70

196618-13-0( オセルタミビル)キーワード:


  • 196618-13-0
  • TAMIFLU
  • OSELTAMIVIR
  • OSTELTAMIVIR
  • Ethyl (3R,4R,5S)-4-acetamido-5-amino-3-(1-ethylpropoxy)-1-cyclohexene-1-carboxylate
  • (3R,5S)-ethyl 4-acetamido-5-amino-3-(pentan-3-yloxy)cyclohex-1-enecarboxylate
  • Oseltamivir (free base)
  • ethyl (3R,4R,5S)-5-aMino-4-acetaMido-3-(pentan-3-yloxy)cyclohex-1-ene-1-carboxylate
  • GOP-A-Flu
  • GS 4104
  • TaMiflu-Free
  • TaMvir
  • (3R,4R,5S)-Ethyl 4-acetamido-5-amino-3-(pentan-3-yloxy)cyclohex-1-enecarboxylate
  • オセルタミビル
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