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マラビロック

マラビロック 化学構造式
376348-65-1
CAS番号.
376348-65-1
化学名:
マラビロック
别名:
マラビロック;マラビロク
英語化学名:
Maraviroc
英語别名:
maroviroc;Celsentri;Maraviroc;Maraviroc API;Maraviroc, >=99%;Maraviroc(UK427857);Maraviroc(Selzentry);Maraviroc(Selzentry, UK-427857);Maraviroc cas 376348-65-1(whatsapp:+8618830163278);4,4-Difluoro-N-((1S)-3-((1R,5S)-3-(3-isopropyl-5-methyl-4H-1,2,4-triazol-4-yl)-8-azabicyclo[3.
CBNumber:
CB71270957
分子式:
C29H41F2N5O
分子量:
513.67
MOL File:
376348-65-1.mol

マラビロック 物理性質

融点 :
79-81°C
貯蔵温度 :
Store at +4°C
溶解性:
DMSO: >30mg/mL
酸解離定数(Pka):
7.3(at 25℃)
外見 :
white powder
光学活性 (optical activity):
[α]-15/D
CAS データベース:
376348-65-1(CAS DataBase Reference)

安全性情報

主な危険性  Xn
Rフレーズ  48/22
Sフレーズ  22-36
WGK Germany  1

マラビロック 価格 もっと(8)

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) W01TOC3756
Maraviroc
376348-65-1 10mg ¥60000 2018-12-26 購入
富士フイルム和光純薬株式会社(wako) W01TOC3756
Maraviroc
376348-65-1 50mg ¥262000 2018-12-26 購入
Sigma-Aldrich Japan PZ0002 マラビロク ≥98% (HPLC)
Maraviroc ≥98% (HPLC)
376348-65-1 25mg ¥108600 2018-12-25 購入
Sigma-Aldrich Japan PZ0002 マラビロク ≥98% (HPLC)
Maraviroc ≥98% (HPLC)
376348-65-1 5mg ¥28800 2018-12-25 購入
富士フイルム和光純薬株式会社(wako) W01TRCM193000 マラビロック
Maraviroc
376348-65-1 25mg ¥40000 2018-12-26 購入

マラビロック 化学特性,用途語,生産方法

化学的特性

Brown Solid

使用

Potent, non-competitive CCR5 receptor antagonist; inhibits binding of HIV viral coat protein gp120. Antiviral

使用

Maraviroc is a CCR5 antagonist for MIP-1α, MIP-1β and RANTES with IC50 of 3.3 nM, 7.2 nM and 5.2 nM, respectively

定義

ChEBI: A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 4,4-difluorocyclohexanecarboxylic acid and the primary amino group of (1S)-3-[(3-exo)-3-(3-isopropyl-5-methyl-4H-1,2,4- riazol-4-yl)-8-azabicyclo[3.2.1]oct-8-yl]-1-phenylpropylamine. An antiretroviral drug, it prevents the interaction of HIV-1 gp120 and chemokine receptor 5 (CCR5) necessary for CCR5-tropic HIV-1 to enter cells.

獲得抵抗性

In most patients (c. 60%) failure of response is associated with the selection of virus that can use CXCR4 as its entry co-receptor. Evidence for the selection of virus that continues to use CCR5 has also been described.

応用例(製薬)

A spirodiketopiperazine formulated as tablets for oral use.

薬物動態学

Oral absorption: c. 33% (300 mg dose)
Cmax 150 mg twice daily: c. 332 μg/L*
Cmin 150 mg twice daily: c. 101 μg/L*
Plasma half-life: c. 13.2 h (30 mg iv administration)
Volume of distribution: c. 194 L
Plasma protein binding: c. 76%
Absorption
The absolute bioavailability of a 100 mg dose is 23% and is predicted to be 33% after a 300 mg dose. Co-administration of a 300 mg tablet and a high-fat meal has resulted in reduced Cmax and AUC by 33% in healthy volunteers. However, because no food restrictions were enacted during clinical trials, maraviroc may be taken with or without food.
Distribution
Animal experiments suggest low CSF concentrations around 10% of free plasma concentrations. It is not known whether it passes into breast milk. A study of genital tract secretions and vaginal tissue in healthy HIV-uninfected female volunteers suggest a concentration in cervicovaginal fluid more than four-fold higher than that in plasma.
Metabolism
It is a substrate for CYP3A4 and P-glycoprotein, but does not appear to inhibit or induce CYP3A4.
Excretion
Seventy-six and 19% of a radiolabeled maraviroc dose were recovered in the feces and urine, respectively.

臨床応用

Treatment of HIV infection (in combination with other antiretroviral drugs) in treatment-experienced patients
On November 20, 2009, the US Food and Drug Administration approved a supplemental new drug application to expand the indication for maraviroc to include combination antiretroviral treatment of treatmentnaive adults infected with CCR5-tropic HIV virus

副作用

There has been some concern that CCR5 blockade may result in decreased immune surveillance and a subsequent increased risk of development of malignancies (e.g. lymphomas). Genetic deficiency of the CCR5 co-receptor is also known to be a risk factor for the development of symptomatic West Nile virus infection. No evidence for an increase in either of these potential risks has so far emerged.
The toxicity profile appears relatively benign. The most common adverse events described so far include diarrhea, fatigue, headache and nausea. In placebo-controlled studies the only differences to emerge were fever (6% versus 4% in the placebo group) and headache (2% versus 6% with placebo). Discontinuation because of adverse events was uncommon and the same in both groups.

マラビロック 上流と下流の製品情報

原材料

準備製品


マラビロック 生産企業

Global( 128)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
Capot Chemical Co.,Ltd.
+86 (0)571-855 867 18
+86 (0)571-858 647 95 sales@capotchem.com China 19953 60
Henan DaKen Chemical CO.,LTD.
+86-371-55531817
info@dakenchem.com CHINA 22049 58
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com CHINA 20786 55
Mainchem Co., Ltd.
+86-0592-6210733
+86-0592-6210733 sales@mainchem.com CHINA 32651 55
Nanjing ChemLin Chemical Industry Co., Ltd.
025-83697070;product@chemlin.com.cn
product@chemlin.com.cn CHINA 3015 60
Hubei Jusheng Technology Co.,Ltd.
86-155-27864001
peter@hubeijusheng.com CHINA 18004 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 10967 58
Biochempartner
0086-13720134139
candy@biochempartner.com CHINA 955 58
Hebei Huanhao Biotechnology Co., Ltd.
86-0311-83975816
86-0311-83975816 lisa@hbhuanhao.com CHINA 668 58
career henan chemical co
+86-371-86658258
sales@coreychem.com CHINA 19990 58

376348-65-1(マラビロック)キーワード:


  • 376348-65-1
  • maroviroc
  • 4,4-Difluoro-N-{(1S)-3-[3-(3-isopropyl-5-methyl-4H-1,2,4-triazol-4-yl)-8-azabicyclo[3.2.1]oct-8-yl]-1-phenylpropyl}cyclohexanecarboxamide
  • Maraviroc(Selzentry)
  • 4,4-difluoro-N-[(1S)-3-[(1R,3R,5S)-3-[3-Methyl-5-(propan-2-yl)-4H-1,2,4-triazol-4-yl]-8-azabicyclo[3.2.1]octan-8-yl]-1-phenylpropyl]cyclohexane-1-carboxaMide
  • Celsentri
  • 4,4-difluoro-N-((1R)-3-(3-(3-isopropyl-5-Methyl-4H-1,2,4-triazol-4-yl)-8-azabicyclo[3.2.1]octan-8-yl)-1-phenylpropyl)cyclohexanecarboxaMide
  • 4,4-difluoro-N-(3-(3-(3-isopropyl-5-Methyl-4H-1,2,4-triazol-4-yl)-8-azabicyclo[3.2.1]octan-8-yl)-1-phenylpropyl)cyclohexanecarboxaMide
  • Maraviroc API
  • 4,4-difluoro-N-((S)-3-((1S,3R,5R)-3-(3-isopropyl-5-Methyl-4H-1,2,4-triazol-4-yl)-8-aza-bicyclo[3.2.1]octan-8-yl)-1-phenylpropyl)cyclohexanecarboxaMide
  • Maraviroc(Selzentry, UK-427857)
  • 4,4-difluoro-N-((S)-3-(3-(3-isopropyl-5-methyl-4H-1,2,4-triazol-4-yl)-8-aza-bicyclo[3.2.1]octan-8-yl)-1-phenylpropyl)cyclohexanecarboxamide
  • 4,4-Difluoro-N-[(1S)-3-[(3-exo)-3-[3-methyl-5-(1-methylethyl)-4H-1,2,4-triazol-4-yl]-8-azabicyclo[3.2.1]oct-8-yl]-1-phenylpropyl]cyclohexanecarboxamide
  • Maraviroc, >=99%
  • 4,4-Difluoro-N-((1S)-3-((1R,5S)-3-(3-isopropyl-5-methyl-4H-1,2,4-triazol-4-yl)-8-azabicyclo[3.
  • Maraviroc
  • Maraviroc(UK427857)
  • 4,4-Difluoro-N-[(1S)-3-[(1R,5S)-3-(3-methyl-5-propan-2-yl-1,2,4-triazol-4-yl)-8-azabicyclo[3.2.1]octan-8-yl]-1-phenylpropyl]cyclohexane-1-carboxamide
  • Maraviroc cas 376348-65-1(whatsapp:+8618830163278)
  • マラビロック
  • マラビロク
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