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アムプレナビル

アムプレナビル 化学構造式
161814-49-9
CAS番号.
161814-49-9
化学名:
アムプレナビル
别名:
アムプレナビル;アンプレナビル
英語化学名:
AMPRENAVIR
英語别名:
PROZEI;141W94;VX 478;KVX-478;AGENERASE;AMPRENAVIR;Angenerase;Amprenavir(KVX-478);AMprenavir(agenerase);141W94, KVX-478, Agenerase, Prozei,
CBNumber:
CB4186139
化学式:
C25H35N3O6S
分子量:
505.63
MOL File:
161814-49-9.mol

アムプレナビル 物理性質

融点 :
72-74°C
貯蔵温度 :
-20°C Freezer
溶解性:
DMSO: soluble20mg/mL, clear
外見 :
powder
色:
white to beige
光学活性 (optical activity):
[α]/D +8 to +12°, c = 0.5 in methanol
InChIKey:
YMARZQAQMVYCKC-OEMFJLHTSA-N

安全性情報

RIDADR  3077
WGK Germany  3
HSコード  29350090

アムプレナビル 価格 もっと(15)

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) W01COBQB-7767 アムプレナビル
Amprenavir
161814-49-9 250mg ¥136800 2018-12-26 購入
富士フイルム和光純薬株式会社(wako) W01COBQB-7767 アムプレナビル
Amprenavir
161814-49-9 100mg ¥68400 2018-12-26 購入
Sigma-Aldrich Japan SML0685 ≥98% (HPLC)
Amprenavir ≥98% (HPLC)
161814-49-9 25mg ¥84700 2018-12-25 購入
Sigma-Aldrich Japan SML0685 ≥98% (HPLC)
Amprenavir ≥98% (HPLC)
161814-49-9 5mg ¥22400 2018-12-25 購入
富士フイルム和光純薬株式会社(wako) W01W0101-2526 アンプレナビル 97.0+% (HPLC)
Amprenavir 97.0+% (HPLC)
161814-49-9 25mg ¥33000 2018-12-26 購入

アムプレナビル 化学特性,用途語,生産方法

外観

白色~うすい褐色, 結晶性粉末~粉末

溶解性

エタノール及びアセトンに溶け、水にほとんど溶けない。

説明

Amprenavir was launched as Agenerase in the US for the treatment of AIDS patients in combination with approved agent antiretroviral nucleoside analogs. It is the fifth non-peptidic inhibitor of HIV-1 protease to be marketed in this indication after the last approved Neflinavir. Amprenavir, designed via a structure-based process, is the smallest molecule in the 《navir》 class and exhibits a reduced peptidic character. An improved process for preparation comprising four steps from a (1S, 2R)-2-hydroxy-3-aminopropylcarbamate has been developed. Amprenavir is a potent inhibitor of HIV-1 aspartyl protease (Ki = 0.6nM), an enzyme required by the virus to cleave pro-form polyproteins to structural proteins during the last stage in the replication process. The compound displays good oral bioavailability in humans and penetrates the CNS, which is an important advantage in long-term treatment. Its plasma half-life is approximately 10h. Treatment with Amprenavir in combination with nucleoside analog reverse transcriptase inhibitors considerably decreases viral load and restores CD4+ T-cell counts in patients with HIV infection.

化学的特性

Off-White to Pale Yellow

Originator

Vertex Pharm (US)

使用

A selective HIV protease inhibitor. An analogue of Ritonavir

使用

Protease inhibitor, anti-HIV agent

brand name

Agenerase (GlaxoSmithKline).

獲得抵抗性

Mutations at position 50, 76 and 84 of the protease enzyme gene are associated with significantly reduced susceptibility.

応用例(製薬)

A synthetic compound formulated as the calcium salt of the oral prodrug fosamprenavir.

薬物動態学

Oral absorption: Not known/available
Cmax 700 mg + ritonavir 100 mg:c. 6.08 mg/L
twice daily
Cmin 700 mg + ritonavir 100 mg:c. 2.12 mg/L
twice daily
Plasma half-life: c. 7.7 h
Volume of distribution: c. 430 L
Plasma protein binding: c. 90%
Absorption
Fosamprenavir is rapidly and almost completely hydrolyzed to amprenavir and inorganic phosphate by cellular phosphatases in the gut epithelium as it is absorbed. Absolute bioavailability has not been established. It can be taken without regard to food.
Distribution
It penetrates moderately well into the CNS. The semen:plasma ratio is negligible. It is not known if it is distributed into breast milk.
Metabolism and excretion
It is extensively metabolized by the cytochrome P450 (CYP) 3A4 enzyme system. Two major metabolites have been identified that appear to result from the oxidation of the tetrahydrofuran and aniline moieties. Around 14% of a dose is eliminated in the urine and 75% in feces, <3% as unchanged drug. Metabolites account for >90% of administered drug found in fecal samples. It should be used with caution and at reduced doses in adults with mild or moderate hepatic impairment; it is contraindicated in patients with severe hepatic impairment.

臨床応用

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

副作用

The most common adverse events in patients receiving boosted fosamprenavir were diarrhea, nausea, headache, fatigue, vomiting and rash. Ritonavir-boosted fosamprenavir is associated with a dyslipidemia profile characteristic of those treated with other protease inhibitors boosted with 200 mg of ritonavir.

使用上の注意

不活性ガス封入

アムプレナビル 上流と下流の製品情報

原材料

準備製品


アムプレナビル 生産企業

Global( 112)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
Capot Chemical Co.,Ltd.
+86 (0)571-855 867 18
+86 (0)571-858 647 95 sales@capotchem.com China 19953 60
Biochempartner
0086-13720134139
candy@biochempartner.com CHINA 956 58
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
Hubei Jusheng Technology Co.,Ltd.
86-188-71490254
peter@hubeijusheng.com CHINA 20229 58
Shanghai Hanxiang Biotechnology Co. Ltd. 15971444841
amber@biochempartner.net China 4995 58
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
3B Pharmachem (Wuhan) International Co.,Ltd. 86-21-50328103 * 801、802、803、804 Mobile:18930552037
86-21-50328109 3bsc@sina.com China 15926 69
Alabiochem Tech.Co., Ltd. 0086-512-58900862; 400-0707-518; 0086-512-56727736
0086-512-56765862 sales@alabiochem.com China 944 59

161814-49-9(アムプレナビル)キーワード:


  • 161814-49-9
  • [(3S)-Oxolan-3-yl] N-[(2S,3R)-4-[(4-aminophenyl)sulfonyl-(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]carbamate
  • N-[(1S,2R)-3-[[(4-AMinophenyl)sulfonyl](2-Methylpropyl)aMino]-2-hydroxy-1-(phenylMethyl)propyl]carbaMic Acid (3S)-Tetrahydro-3-furanyl Ester
  • KVX-478
  • AGENERASE
  • AMprenavir(agenerase)
  • Amprenavir(KVX-478)
  • AMPRENAVIR
  • 141W94
  • PROZEI
  • 141W94, KVX-478, Agenerase, Prozei,
  • Carbamic acid, (1S,2R)-3-(4-aminophenyl)sulfonyl(2-methylpropyl)amino-2-hydroxy-1-(phenylmethyl)propyl-, (3S)-tetrahydro-3-furanyl ester
  • Angenerase
  • Carbamic acid, [3-[[(4-aminophenyl)sulfonyl](2-methylpropyl)amino]-2-hydroxy-1-(phenylmethyl)propyl]-, tetrahydro-3-furanyl ester, [3S-[3R*(1R*,2S*)]]-
  • VX 478
  • アムプレナビル
  • アンプレナビル
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