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ロピナビル

ロピナビル 化学構造式
192725-17-0
CAS番号.
192725-17-0
化学名:
ロピナビル
别名:
ロピナビル;ロピナビル (JAN)
英語化学名:
Lopinavir
英語别名:
Koletr;Koletra;ABT 378;Aluviran;LOPINAVIR;A 157378.0;ABT-378 whatsapp;Lopinavir (350 mg);Lopinavir (ABT-378);Lopinavir for system suitability
CBNumber:
CB3663640
化学式:
C37H48N4O5
分子量:
628.8
MOL File:
192725-17-0.mol

ロピナビル 物理性質

融点 :
124-127°C
貯蔵温度 :
Hygroscopic, -20°C Freezer, Under inert atmosphere
溶解性:
DMSO: soluble20mg/mL, clear
外見 :
powder
色:
white to beige
光学活性 (optical activity):
[α]/D -20 to -27°, c = 0.4 in methanol
安定性::
Hygroscopic
CAS データベース:
192725-17-0(CAS DataBase Reference)

安全性情報

RIDADR  3077
HSコード  29335990

ロピナビル 価格 もっと(13)

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) W01COBQJ-3559 ロピナビル
Lopinavir
192725-17-0 1g ¥79200 2018-12-26 購入
富士フイルム和光純薬株式会社(wako) W01COBQJ-3559 ロピナビル
Lopinavir
192725-17-0 5g ¥273600 2018-12-26 購入
Sigma-Aldrich Japan PHR1927 Pharmaceutical Secondary Standard; Certified Reference Material
Lopinavir Pharmaceutical Secondary Standard; Certified Reference Material
192725-17-0 1g ¥42500 2018-12-25 購入
Sigma-Aldrich Japan 1370101 United States Pharmacopeia (USP) Reference Standard
Lopinavir United States Pharmacopeia (USP) Reference Standard
192725-17-0 350mg ¥249300 2018-12-25 購入
富士フイルム和光純薬株式会社(wako) W01LKTL5862 ロピナビル
Lopinavir
192725-17-0 5g ¥116900 2018-12-26 購入

ロピナビル 化学特性,用途語,生産方法

効能

抗ウイルス薬, HIVプロテアーゼ阻害薬

説明

Lopinavir, the sixth HIV protease inhibitor in the “navir” class, was launched in coformulation with ritonavir, another HIV protease inhibitor already marketed (Abbott, 1996); this original formulation was introduced as Kaletra for use in combination with either nucleoside or non-nucleoside reverse transcriptase inhibitors for the treatment of AIDS in adults and children. Lopinavir is a peptidomimetic compound with a structural core identical to that of ritonavir, on which terminal groups, particularly a modified valine, were introduced by peptide coupling procedures. Lopinavir is a potent competitive inhibitor of HIV-I protease exhibiting high potential against ritonavir-resistant mutations. In several animal species, pharmacokinetic studies with the lopinavirlritonavir association showed that the modest properties of lopinavir were significantly improved in presence of ritonavir, in terms of Cmax and duration of action. Ritonavir inhibits the P450 isoenzyme CYP3A4 and the human liver microsomal metabolism of lopinavir, so strongly amplifying plasma levels of this latter component. In AIDS patients, the plasma HIV RNA level was considerably reduced and the CD4+ T-cell counts increased after administration of lopinavir combined with relatively small doses of ritonavir. Kaletra is intended to be used jointly with other antiretroviral agents.

化学的特性

White Crystalline Solid

Originator

Abbott (US)

使用

A selective HIV protease inhibitor. An analogue of Ritonavir. Antiviral.

使用

Lopinavir is a potent HIV protease inhibitor with Ki of 1.3 pM

定義

ChEBI: A dicarboxylic acid amide in which a parent structure of amphetamine is substituted on nitrogen by a (2,6-dimethylphenoxy)acetyl group and on the carbon alpha to nitrogen by a (1S,3S)-1-hydroxy-3-{[(2S)-3- ethyl-2-(2-oxotetrahydropyrimidin-1(2H)-yl)butanoyl]amino}-4-phenylbutyl group. An antiretroviral of the protease inhibitor class. It is used against HIV infections as a fixed-dose combination with another protease inhibitor, ritonavir.

brand name

Kaletra

抗菌性

Lopinavir is active against HIV-1 and HIV-2.

獲得抵抗性

Significant resistance to the antiretroviral efficacy of ritonavirbooted lopinavir occurs as a result of amino acid substitutions at positions 32, 47 and 82 in the protease region. Protease inhibitor resistance is uncommon in patients identified with early failure of combination therapy with ritonavir boostedlopinavir and nucleotide reverse transcriptase inhibitors.

一般的な説明

Lopinavir is a protease inhibitor that has been approved foruse in combination with ritonavir for patients with HIV whohave not responded to other treatment modalities. Lopinaviris used in excess over ritonavir. Ritonavir at amounts givenhas no antiretroviral activity, Ritonavir inhibits lopinavir’smetabolism by CYP3A4, causing a higher level of lopinavirin the system. The combination is the first protease inhibitorapproved for patients as young as 6 months of age.

応用例(製薬)

A synthetic compound, co-formulated with ritonavir for oral administration. In this formulation, ritonavir functions to inhibit the metabolic clearance of lopinavir, and does not contribute to the antiretroviral activity.

薬物動態学

Oral absorption: Not known/available
Cmax 400 mg + ritonavir 100 mg twice daily: c. 9.6 mg/L
Cmin 400 mg + ritonavir 100 mg twice daily: c. 5.5 mg/L
Plasma half-life: c. 5–6 h
Volume of distribution: Not known/available
Plasma protein binding: c. 98–99%
Absorption and distribution
The absorption of lopinavir–ritonavir in capsule or liquid form is favorably affected by the presence of food, particularly if high in fat. The CNS penetration is good. It has a semen:plasma ratio of 0.07. It is distributed into breast milk.
Metabolism
Lopinavir is extensively metabolized by the CYP3A4 system, but this is inhibited by ritonavir.
Excretion
Over an 8-day period after single dosing with the combined formulation, around 10% and 83% of the administered dose is recovered in urine and feces, respectively. Less than 3% of the dose is recovered as unchanged drug in urine and 20% in feces. In mild to moderate hepatic impairment, an increase in exposure of approximately 30% is observed, but is probably not clinically relevant. It should be avoided in severe hepatic impairment.

臨床応用

Treatment of HIV infection (in combination with ritonavir and other antiretroviral agents)

副作用

The most common adverse events seen in trials of complex antiretroviral regimens were diarrhea, nausea, headache, fatigue, vomiting and rash. Ritonavir-boosted lopinavir is associated with a dyslipidemia profile characteristic of those treated with other protease inhibitors boosted with 200 mg of ritonavir.

ロピナビル 上流と下流の製品情報

原材料

準備製品


ロピナビル 生産企業

Global( 195)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 19918 60
Henan DaKen Chemical CO.,LTD.
+86-371-55531817
info@dakenchem.com CHINA 21968 58
Beijing Cooperate Pharmaceutical Co.,Ltd.
+86-10-60279497 +86(0)15646567669
+86-10-60279497 sales01@cooperate-pharm.com CHINA 1530 55
Hebei Jiangkai Trading Co., Ltd
0086-17197824289/17197824028
alice@hbjkai.com CHINA 274 58
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com CHINA 20680 55
Mainchem Co., Ltd.
+86-0592-6210733
+86-0592-6210733 sales@mainchem.com CHINA 32457 55
PI & PI BIOTECH INC.
020-81716320
020-81716319 Sales@pipitech.com CHINA 2543 55
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 24001 58

192725-17-0(ロピナビル)キーワード:


  • 192725-17-0
  • (aS)-N-[(1S,3S,4S)-4-[[2-(2,6-Dimethylphenoxy)acetyl]amino]-3-hydroxy-5-phenyl-1-(phenylmethyl)pentyl]tetrahydro-α-(1-methylethyl)-2-oxo-1(2H)-Pyrimidineacetamide
  • Koletra
  • (2S)-N-[(2S,4S,5S)-5-[[2-(2,6-dimethylphenoxy)acetyl]amino]-4-hydroxy-1,6-diphenyl-hexan-2-yl]-3-methyl-2-(2-oxo-1,3-diazinan-1-yl)butanamide
  • Lopinavir (ABT-378)
  • Lopinavir (350 mg)
  • (αS)-N-[(1S,3S,4S)-4-[[2-(2,6-DiMethylphenoxy)acetyl]aMino]-3-hydroxy-5-phenyl-1-(phenylMethyl)pentyl]tetrahydro-α-(1-Methylethyl)-2-oxo-1(2H)-pyriMidineacetaMide
  • (2S)-N-[(2S,4S,5S)-5-[2-(2,6-diMethylphenoxy)acetaMido]-4-hydroxy-1,6-diphenylhexan-2-yl]-3-Methyl-2-(2-oxo-1,3-diazinan-1-yl)butanaMide
  • (S)-N-((2R,4S,5S)-5-(2-(2,6-Dimethylphenoxy)acetamido)-4-hydroxy-1,6-diphenyl-hexn-2-yl)-3-methyl
  • N-((2S,4S,5S)-5-(2-(2,6-DiMethylphenoxy)acetaMido)-4-hydroxy-1,6-diphenylhexan-2-yl)-3-Methyl-2-(2-oxotetrahydropyriMidin-1(2H)-yl)butanaMide
  • (S)-N-((2S,4S,5S)-5-(2-(2,6-dimethylphenoxy)acetamido)-4-hydroxy-1,6-diphenylhexan-2-yl)-3-methyl-2-(2-oxo-tetrahydropyrimidin-1(2H)-yl)butanamide
  • Lopinavir for system suitability
  • Lopinavir for peak identification
  • (S)-N-((2R,4S,5S)-5-(2-(2,6-Dimethylphenoxy)acetamido)-4-hydroxy-1,6-diphenyl-hexn-2-yl)-3-met
  • ABT-378 whatsapp
  • LOPINAVIR
  • (2s)-n-[(2r,4s,5s)-5-[[2-(2,6-dimethylphenoxy)acetyl]amino]-4-hydroxy-1,6-diphenyl-hexan-2-yl]-3-methyl-2-(2-oxo-1,3-diazinan-1-yl)butanamide
  • (aS)-N-[(1S,3S,4S)-4-[[2-(2,6-Dimethylphenoxy)acetyl]amino]-3-hydroxy-5-phenyl-1-(phenylmethyl)pentyl]tetrahydro-a-(1-methylethyl)-2-oxo-1(2H)-Pyrimidineacetamide
  • A 157378.0
  • ABT 378
  • Aluviran
  • Koletr
  • Lopinavir, 99%, HIV protease inhibitor
  • ロピナビル
  • ロピナビル (JAN)
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