ラルテグラビル

ラルテグラビル 化学構造式
518048-05-0
CAS番号.
518048-05-0
化学名:
ラルテグラビル
别名:
ラルテグラビル;N-(4-フルオロベンジル)-1,6-ジヒドロ-5-ヒドロキシ-1-メチル-2-[1-メチル-1-[(5-メチル-1,3,4-オキサジアゾール-2-イル)カルボニルアミノ]エチル]-6-オキソピリミジン-4-カルボアミド;N-(4-フルオロベンジル)-1,6-ジヒドロ-5-ヒドロキシ-1-メチル-2-[1-メチル-1-[(5-メチル-1,3,4-オキサジアゾール-2-イル)カルボニルアミノ]エチル]-6-オキソ-4-ピリミジンカルボアミド;N-[(4-フルオロフェニル)メチル]-5-ヒドロキシ-1-メチル-2-{2-[(5-メチル-1,3,4-オキサジアゾール-2-イル)ホルムアミド]プロパン-2-イル}-6-オキソ-1,6-ジヒドロピリミジン-4-カルボキサミド
英語名:
Raltegravir
英語别名:
CS-1889;Raltegravir;Reg column wei;Raltegravir(R&D);Raltegravir, >=99%;Raltegravir USP/EP/BP;Raltegravir(free base);Raltegravir (free base) API;MK-0518 518048-05-0 CAS NO.518048-05-0;Raltegravir-d4Q: What is Raltegravir-d4 Q: What is the CAS Number of Raltegravir-d4
CBNumber:
CB61456530
化学式:
C20H21FN6O5
分子量:
444.42
MOL File:
518048-05-0.mol

ラルテグラビル 物理性質

融点 :
216 °C(Solv: isopropanol (67-63-0))
比重(密度) :
1.46±0.1 g/cm3(Predicted)
貯蔵温度 :
-20°C Freezer
溶解性:
DMSO(微量)、メタノール(微量)
酸解離定数(Pka):
4.50±1.00(Predicted)
外見 :
個体
色:
ホワイトからライトベージュ
CAS データベース:
518048-05-0(CAS DataBase Reference)
安全性情報
  • リスクと安全性に関する声明
  • 危険有害性情報のコード(GHS)
有毒物質データの 518048-05-0(Hazardous Substances Data)
絵表示(GHS) GHS hazard pictograms
注意喚起語 警告
危険有害性情報
コード 危険有害性情報 危険有害性クラス 区分 注意喚起語 シンボル P コード
H315 皮膚刺激 皮膚腐食性/刺激性 2 警告 GHS hazard pictograms P264, P280, P302+P352, P321,P332+P313, P362
H319 強い眼刺激 眼に対する重篤な損傷性/眼刺激 性 2A 警告 GHS hazard pictograms P264, P280, P305+P351+P338,P337+P313P
注意書き
P280 保護手袋/保護衣/保護眼鏡/保護面を着用するこ と。
P302+P352 皮膚に付着した場合:多量の水と石鹸で洗うこと。
P305+P351+P338 眼に入った場合:水で数分間注意深く洗うこと。次にコ ンタクトレンズを着用していて容易に外せる場合は外す こと。その後も洗浄を続けること。
P332+P313 皮膚刺激が生じた場合:医師の診断/手当てを受けるこ と。
P337+P313 眼の刺激が続く場合:医師の診断/手当てを受けること。

ラルテグラビル 価格 もっと(5)

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) W01COBQA-7626 ラルテグラビル
Raltegravir
518048-05-0 250mg ¥64800 2021-03-23 購入
富士フイルム和光純薬株式会社(wako) W01COBQA-7626 ラルテグラビル
Raltegravir
518048-05-0 1g ¥162000 2021-03-23 購入
Sigma-Aldrich Japan SML3670 ≥98% (HPLC)
Raltegravir ≥98% (HPLC)
518048-05-0 10MG ¥11300 2024-03-01 購入
Sigma-Aldrich Japan SML3670 ≥98% (HPLC)
Raltegravir ≥98% (HPLC)
518048-05-0 50MG ¥45400 2024-03-01 購入
富士フイルム和光純薬株式会社(wako) W01MAS125346 ラルテグラビル
Raltegravir
518048-05-0 1g ¥926600 2021-03-23 購入

ラルテグラビル 化学特性,用途語,生産方法

効能

抗ウイルス薬, HIVインテグラーゼ阻害薬

説明

Joining maraviroc as a unique approach to battling HIV-1, raltegravir, an inhibitor of HIV-1 integrase, represents the first in its class to be developed and launched as a combination treatment with other antiretroviral agents (NRTIs, NNRTIs, and PIs). HIV-1 integrase is essential for replication of the virus as a virally encoded enzyme that integrates the viral DNA into the genome of the host cell. Inhibition of HIV-1 integrase prevents the two-step process of endonucleolytic removal of the terminal dinucleotide from each 3′end of the viral DNA followed by the covalent integration of the viral DNA, at these modified 3′ends, into the host DNA, thereby representing a viable intervention in the viral life cycle. In vitro, raltegravir inhibited the strand transfer activity of HIV-1 integrase with an IC50 of 2–7nM with > 1,000-fold selectivity over other phosphoryltransferases. In addition, its in vitro IC95 for HIV-1 in 10% fetal bovine serum and 50% human serum was 19 and 33 nM, respectively. Raltegravir was well tolerated with no dose-related toxicities and a safety profile comparable to placebo. The most common clinical adverse events were diarrhea, nausea, vomiting, fatigue, headache, flushing, pruritus, and injection-site reactions.

使用

Raltegravir (MK-0518, Isentress) is a potent integrase (IN) inhibitor for WT and S217Q PFV IN with IC50 of 90 nM and 40 nM, respectively.

獲得抵抗性

Several characteristic mutations leading to typical amino acid exchanges have been characterized in cell culture studies and confirmed in clinical trial participants with virological failure while receiving raltegravir in combination with other antiretrovirals. Virological failure has generally been associated with mutations at one of three residues – Y143, Q148 or N155 – usually in combination with at least one other mutation.

応用例(製薬)

Formulated as the potassium salt for oral administration.

薬物動態学

Oral absorption: Not known/available
Cmax 400 mg twice daily: c. 2.17 mg/L
Plasma half-life: c. 9 h
Volume of distribution: Not known/available
Plasma protein binding: c. 83%
Absorption and distribution
It may be administered without regard to food. There are few data regarding its capacity to penetrate into genital secretions or breast milk. A study of 25 HIV-infected individuals receiving raltegravir as a component of combination antiretroviral therapy found that 24 had detectable levels and that 50% of these reached a level exceeding the 95% inhibitory concentration reported to inhibit HIV-1 strains fully susceptible to integrase inhibition.
Metabolism and excretion
It is not a substrate, and does not appear to inhibit or induce the cytochrome P450 enzyme complex. It is primarily metabolized through hepatic glucuronidation mediated by the UGT-1A1 enzyme. It is excreted in the feces (51%) and the urine (32%) as unaltered compound and its glucuronide. There are no recommended dose adjustments for weight, sex and race, or for hepatic or renal insufficiency. The pharmacokinetic handling in children has not been determined.

臨床応用

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

副作用

Its toxicity profile to date is remarkably benign. Clinical trial participants experienced similar types and frequencies of adverse events as those receiving placebo. The most frequently reported adverse events were nausea, diarrhea and headache and were mostly mild to moderate in intensity. Myopathy, rhabdomyolysis and elevations of creatinine phosphokinase have been noted in a few trial participants and it should be used cautiously in combination with drugs associated with muscle toxicity.

ラルテグラビル 上流と下流の製品情報

原材料

準備製品


ラルテグラビル 生産企業

Global( 267)Suppliers
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ラルテグラビル  スペクトルデータ(1HNMR)


518048-05-0(ラルテグラビル)キーワード:


  • 518048-05-0
  • N-((4-Fluorophenyl)methyl)-1,6-dihydro-5-hydroxy-1-methyl-2-(1-methyl-1-(((5-methyl-1,3,4-oxadiazol-2
  • Raltegravir N-(2-(4-(4-Fluorobenzylcarbamoyl)-5-hydroxy-1-methyl-6-oxo-1,6-dihydropyrimidin-2-yl)propan-2-yl)-5-methyl-1,3,4-oxadiazole-2-carboxamide
  • Raltegravir (free base) API
  • Raltegravir, >=99%
  • N-((4-Fluorophenyl)methyl)-1,6-dihydro-5-hydroxy-1-methyl-2-(1-methyl-1-(((5-methyl-1,3,4-oxadiazol-2-yl)carbonyl)amino)ethyl)-6-oxo-4-pyrimidinecarboxamide
  • N-(2-(4-(4-Fluorobenzylcarbamoyl)-5-hydroxy-1-methyl-6-oxo-1,6-dihydropyrimidin-2-yl)propan-2-yl)-5-methyl-1,3,4-oxadiazole-2-carboxamide
  • Raltegravir
  • N-(2-(4-(4-Fluorobenzylcarbamoyl)-5-hydroxy-1-methyl-6-oxo-1,6-dihydropyrimidin-2-yl)p
  • Raltegravir(R&D)
  • Raltegravir(free base)
  • N-(4-fluorobenzyl)-5-hydroxy-1-methyl-2-(2-(2-methyl-1,3,4-oxadiazole-5-carboxamido)propan-2-yl)-6-oxo-1,6-dihydropyrimidine-4-carboxamide
  • N-((4-Fluorophenyl)methyl)-1,6-dihydro-5-hydroxy-1-methyl-2-(1-methyl-1-(((5-methyl-1,3,4-oxadiazol-2-yl)carbonyl)am
  • MK-0518 518048-05-0 CAS NO.518048-05-0
  • CS-1889
  • 4-Pyrimidinecarboxamide, N-[(4-fluorophenyl)methyl]-1,6-dihydro-5-hydroxy-1-methyl-2-[1-methyl-1-[[(5-methyl-1,3,4-oxadiazol-2-yl)carbonyl]amino]ethyl]-6-oxo-
  • N-[2-[4-[(4-fluorophenyl)methylcarbamoyl]-5-hydroxy-1-methyl-6-oxopyrimidin-2-yl]propan-2-yl]-5-methyl-1,3,4-oxadiazole-2-carboxamide
  • Reg column wei
  • Raltegravir USP/EP/BP
  • Raltegravir-13Cd3Q: What is Raltegravir-13Cd3 Q: What is the CAS Number of Raltegravir-13Cd3
  • Raltegravir-d4Q: What is Raltegravir-d4 Q: What is the CAS Number of Raltegravir-d4
  • N-[(4-fluorophenyl)methyl]-5-hydroxy-1-methyl-2-{2-[(5-methyl-1,3,4-oxadiazol-2-yl)formamido]propan-2-yl}-6-oxo-1,6-dihydropyrimidine-4-carboxamide
  • N-(2-(4-((4-Fluorobenzyl)carbamoyl)-5-hydroxy-1-methyl-6-oxo-1,6-dihydropyrimidin-2-yl)propan-2-yl)-5-methyl-1,3,4-oxadiazol-2-carboxamide
  • ラルテグラビル
  • N-(4-フルオロベンジル)-1,6-ジヒドロ-5-ヒドロキシ-1-メチル-2-[1-メチル-1-[(5-メチル-1,3,4-オキサジアゾール-2-イル)カルボニルアミノ]エチル]-6-オキソピリミジン-4-カルボアミド
  • N-(4-フルオロベンジル)-1,6-ジヒドロ-5-ヒドロキシ-1-メチル-2-[1-メチル-1-[(5-メチル-1,3,4-オキサジアゾール-2-イル)カルボニルアミノ]エチル]-6-オキソ-4-ピリミジンカルボアミド
  • N-[(4-フルオロフェニル)メチル]-5-ヒドロキシ-1-メチル-2-{2-[(5-メチル-1,3,4-オキサジアゾール-2-イル)ホルムアミド]プロパン-2-イル}-6-オキソ-1,6-ジヒドロピリミジン-4-カルボキサミド
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