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アタザナビル

アタザナビル 化学構造式
198904-31-3
CAS番号.
198904-31-3
化学名:
アタザナビル
别名:
アタザナビル
英語化学名:
Atazanavir
英語别名:
Atv;atazanvir;EOS-60363;Atazanavir;Aids057755;Aids-057755;Atazanavir, >=99%;Atazanavir iMpurity;Atazanavir free base;Atazanavir Enantiomer
CBNumber:
CB0500863
化学式:
C38H52N6O7
分子量:
704.87
MOL File:
198904-31-3.mol

アタザナビル 物理性質

融点 :
207-2090C
比旋光度 :
D -47° (c = 1 in ethanol)
貯蔵温度 :
-20°C Freezer
外見 :
powder
色:
white to beige
CAS データベース:
198904-31-3

安全性情報

有毒物質データの 198904-31-3(Hazardous Substances Data)

アタザナビル 価格 もっと(4)

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) W01TRCA790051 アタザナビル
Atazanavir
198904-31-3 5mg ¥23800 2018-12-26 購入
富士フイルム和光純薬株式会社(wako) W01TRCA790051 アタザナビル
Atazanavir
198904-31-3 50mg ¥137500 2018-12-26 購入
Sigma-Aldrich Japan SML1796 ≥98% (HPLC)
Atazanavir ≥98% (HPLC)
198904-31-3 5mg ¥18900 2018-12-25 購入
Sigma-Aldrich Japan SML1796 ≥98% (HPLC)
Atazanavir ≥98% (HPLC)
198904-31-3 25mg ¥76200 2018-12-25 購入

アタザナビル 化学特性,用途語,生産方法

用途

アタザナビル(Atazanavir)は商標名のレイアタッツ(Reyataz)として販売されており、抗レトロウィルス薬としてHIV/エイズの治療と予防に用いられる医薬品である。一般的に他の抗レトロウィルス薬との併用が勧められる。

化学的特性

Crystalline Solid

使用

Atazanavir is a novel azapeptide protease inhibitor (PI)

使用

enzyme inhibitor

使用

Atazanavir is a novel azapeptide HIV protease inhibitor (PI). Antiviral.

定義

ChEBI: A heavily substituted carbohydrazide that is an antiretroviral drug of the protease inhibitor (PI) class used to treat infection of human immunodeficiency virus (HIV).

使用

Atazanavir is an inhibitor of HIV-1 protease (EC50 = 2.6 nM). In isolated cells, it has additive to moderately synergistic antiviral effects when combined with other antiretroviral drugs. As a result, it is commonly used in vivo in combination therapy for HIV-1 infection. Atazanavir competitively inhibits UDP-gluronosyltransferase, which conjugates bilirubin for clearance, leading to hyperbilirubinemia in a significant portion of those receiving atazanavir therapy.

brand name

Reyataz (Bristol-Myers Squibb).

獲得抵抗性

Mutations at positions 50 (I50L), 84 (I84V) and 88 (N88S) of the protease gene are associated with resistance.

一般的な説明

Atazanavir is an antiretroviral agent that has been approvedby the FDA for use in combination with other anti-RTagents for the treatment of HIV infections. The drug is alwaysused in combination with RT inhibitors.

応用例(製薬)

An azapeptide formulated as the sulfate for oral use.

薬物動態学

Oral absorption: c. 68%
Cmax 400 mg once daily: c. 3.15 μg/L
300 mg + ritonavir 100 mg once daily: c. 4.47 μg/L
Cmin 400 mg once daily: c. 0.27 μg/L
300 mg + ritonavir 100 mg once daily: c. 0.65 μg/L
Plasma half-life: c. 8.6 h (300 mg+ ritonavir 100 mg)
Volume of distribution: c. Not known/available
Plasma protein binding: c. 86%
Absorption
Administration with food enhances bioavailability and reduces pharmacokinetic variability. Absorption is dependent on gastric pH. It should be given separately from proton-pump inhibitors or H2-receptor antagonists. Buffered or entericcoated formulations should be given (with food) 2 h before or 1 h after co-administration of didanosine.
Distribution
It penetrates moderately well into the CNS. The semen:plasma ratio is 0.11–4.42. It is distributed into breast milk.
Metabolism
It is extensively metabolized by CYP3A4. Administration with ritonavir prevents metabolization and enhances the pharmacokinetic profile.
Excretion
Following a single 400 mg dose, 79% and 13% of the dose was recovered in the feces and urine, respectively. It should be used with caution in the presence of mild hepatic impairment and should not be used in patients with more severe hepatic impairment.

臨床応用

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

副作用

The most common adverse reactions (≥2%) are nausea, jaundice/ scleral icterus, rash, headache, abdominal pain, vomiting, insomnia, peripheral neurological symptoms, dizziness, myalgia, diarrhea, depression and fever.

アタザナビル 上流と下流の製品情報

原材料

準備製品


アタザナビル 生産企業

Global( 142)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 19954 60
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
PI & PI BIOTECH INC.
020-81716320
020-81716319 Sales@pipitech.com CHINA 2548 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
J & K SCIENTIFIC LTD. 400-666-7788 +86-10-82848833
+86-10-82849933 jkinfo@jkchemical.com;market6@jkchemical.com China 96815 76
Alabiochem Tech.Co., Ltd. 0086-512-58900862; 400-0707-518; 0086-512-56727736
0086-512-56765862 sales@alabiochem.com China 944 59
Chembest Research Laboratories Limited +86(0)21-20908456
+86(0)21-58180499 sales@biochembest.com; market@biochembest.com China 6013 61

198904-31-3(アタザナビル)キーワード:


  • 198904-31-3
  • atazanvir
  • Atazanavir, >=99%
  • Atazanavir Enantiomer
  • Atazanavir Isomer Impurity
  • Atazanavir Isomer Impurity 1
  • Atazanavir Isomer Impurity 2
  • Atazanavir Isomer Impurity 3
  • Atazanavir Intermediate Impurity 1
  • Atazanavir Intermediate Impurity 2
  • Atazanavir Intermediate Impurity 3
  • Atazanavir Intermediate Impurity 4
  • methyl((5S,10S,11S,14S)-11-benzyl-5-(tert-butyl)-10-hydroxy-15,15-dimethyl-3,6,13-trioxo-8-(4-(pyridin-2-yl)benzyl)-2-oxa-4,7,8,12-tetraazahexadecan-14-yl)carbamate
  • Methyl N-[(2S)-1-[[(2S,3S)-3-hydroxy-4-[[[(2S)-2-(methoxycarbonylamino)-3,3-dimethylbutanoyl]a
  • EOS-60363
  • ATAZANAVIR, BISULFATE SALT
  • Atazanavir
  • (3S,8S, 9S, 12S)-2,5,6,13-Pentaazatetradecanedioic Acid
  • 3,12-Bis(1,1-dimethylethyl)-8-hydroxy-4,11-dioxo-9-(phenylmethyl)-6-[[4-(2-pyridinyl)phenyl]methyl]-dimethyl Ester
  • Methyl N-[(2S)-1-[[(2S,3S)-3-hydroxy-4-[[[(2S)-2-(methoxycarbonylamino)-3,3-dimethylbutanoyl]amino]-[(4-pyridin-2-ylphenyl)methyl]amino]-1-phenylbutan-2-yl]amino]-3,3-dimethyl-1-oxobutan-2-yl]carbamate
  • (2S)-N-(3-{[(2S)-2-(Methoxycarbonylamino)-3,3-dimethylbutanoylamino][(4-(2-pyridyl)phenyl)methyl]amino}(1S,2S)-2-hydroxy-1-benzylpropyl)-2-(methoxycarbonylamino)-3,3-dimethylbutanamide
  • 229975-97-7 (Sulfate 1:1)
  • Aids057755
  • Aids-057755
  • Atv
  • Atazanavir & Atazanavir Sulfate
  • BMS-232632(Atazanavir)
  • Atazanavir(BMS-232632)
  • Methyl N-[(2S)-1-[[(2S,3S)-3-hydroxy-4-[[[(2S)-2-(MethoxycarbonylaMino)-
  • Atazanavir free base
  • Atazanavir iMpurity
  • アタザナビル
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