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リトナビル

リトナビル 化学構造式
155213-67-5
CAS番号.
155213-67-5
化学名:
リトナビル
别名:
リトナビル;リトナビル (JAN)
英語化学名:
Ritonavir
英語别名:
Norvi;Norvir;RITONA;CS-477;ABT-538;A 84538;Ritonavi;RITONAVIR;litonavir;NSC 693184
CBNumber:
CB0119429
化学式:
C37H48N6O5S2
分子量:
720.94
MOL File:
155213-67-5.mol

リトナビル 物理性質

融点 :
120-122°C
沸点 :
947.0±65.0 °C(Predicted)
比重(密度) :
1.239±0.06 g/cm3(Predicted)
闪点 :
2℃
貯蔵温度 :
room temp
溶解性:
DMSO: soluble10mg/mL (clear solution, warmed)
外見 :
powder
酸解離定数(Pka):
11.47±0.46(Predicted)
色:
white to beige
水溶解度 :
5mg/L(ms)
Merck :
14,8238
InChIKey:
NCDNCNXCDXHOMX-XGKFQTDJSA-N
CAS データベース:
155213-67-5(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)
主な危険性  Xi,Xn
Rフレーズ  36/38-20/21/22-41
Sフレーズ  26-37/39-36/37-39
RIDADR  UN 1648 3 / PGII
WGK Germany  3
RTECS 番号 XA5310000
HSコード  29341000
有毒物質データの 155213-67-5(Hazardous Substances Data)
絵表示(GHS)
注意喚起語 Danger
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
H225 引火性の高い液体および蒸気 引火性液体 2 危険 P210,P233, P240, P241, P242, P243,P280, P303+ P361+P353, P370+P378,P403+P235, P501
H319 強い眼刺激 眼に対する重篤な損傷性/眼刺激 性 2A 警告 P264, P280, P305+P351+P338,P337+P313P
注意書き
P210 熱/火花/裸火/高温のもののような着火源から遠ざ けること。-禁煙。
P261 粉じん/煙/ガス/ミスト/蒸気/スプレーの吸入を避ける こと。
P280 保護手袋/保護衣/保護眼鏡/保護面を着用するこ 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。

リトナビル 価格 もっと(20)

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) W01TRCR535000 リトナビル
Ritonavir
155213-67-5 5mg ¥16300 2021-03-23 購入
富士フイルム和光純薬株式会社(wako) W01FLC358080
1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[(2S)-3-methyl-2-{[methyl({[2-(propan-2-yl)-1,3-thiazol-4-yl]methyl})carbamoyl]amino}butanamido]-1,6-diphenylhexan-2-yl]carbamate
155213-67-5 1g ¥127500 2021-03-23 購入
東京化成工業 R0116 リトナビル >98.0%(HPLC)(N)
Ritonavir >98.0%(HPLC)(N)
155213-67-5 200mg ¥7700 2021-03-23 購入
東京化成工業 R0116 リトナビル >98.0%(HPLC)(N)
Ritonavir >98.0%(HPLC)(N)
155213-67-5 1g ¥25200 2021-03-23 購入
Sigma-Aldrich Japan Y0000714 European Pharmacopoeia (EP) Reference Standard
European Pharmacopoeia (EP) Reference Standard
155213-67-5 ¥35200 2021-03-23 購入

リトナビル 化学特性,用途語,生産方法

外観

白色~ほとんど白色、結晶性粉末~粉末

溶解性

メタノール及びエタノールに溶けやすく、水にほとんど溶けない。

用途

HIV プロテアーゼ阻害剤です。 タンパク質前駆体の開裂に関与する HIV プロ テアーゼを阻害することにより、成熟ウイル スの産生を阻害します。

効能

抗ウイルス薬, HIVプロテアーゼ阻害薬

商品名

ノービア (アッヴィ)

使用上の注意

アルゴン封入

説明

Norvir was launched in Germany, the UK and US for treatment of advanced HIV in combination with antiretroviral nucleoside analogs in a record 72 days by the FDA. It is an inhibitor of HIV aspartic protease which is critical in the processing of a propeptide into the gag, gag-pol gene products and the protease itself. This inhibition results in the release of non-infectous immature virus particles. It is greater than 500-fold more selective for viral aspartic protease than the human version, has good oral bioavailability and may increase the bioavailability of other protease inhibitors. Ritonavir was able to increase the CD4 and CD8 lymphocyte count as well as reduce viral RNA. It is more potent than saqunavir and comparible in potency to zidovudine and lamivudine.Ritonavir.jpg

説明

Ritonavir is an HIV protease inhibitor. It inhibits recombinant HIV-1 protease by 79% when used at a concentration of 0.5 nM. It inhibits HIV-13B-induced cell death in MT-4 human T cell leukemia cells (EC50 = 25 nM) as well as cell death induced by HIV-1LAI, HIV-2ROD, and HIV-2EHO in human MT-2 cells (IC50s = 0.045, 0.13, and 0.24 μM, respectively). Ritonavir also inhibits the cytochrome P450 (CYP) isoform CYP3A (IC50 = 0.14 μM). It inhibits CYP-mediated oxidative metabolism of the HIV protease inhibitors saquinavir (Item No. 9001893), indinavir (Item No. 15150), nelfinavir (Item No. 15144), and amprenavir (Item No. 15369) in rat and human liver microsomes in a concentration-dependent manner. Ritonavir (10 mg/kg) also prevents decreases in plasma levels of these four compounds in rats. Formulations containing ritonavir have been used in the treatment of HIV-1 infection.

化学的特性

White or almost white powder.

Originator

Abbott (USA)

使用

Protease inhibitor; antiviral (HIV).

使用

Ritonivir is an HIV protease inhibitor (EC50 = 25 nM) that also inhibits CYP3A4, the primary cytochrome P450 isoform that metabolizes protease inhibitors. Through CYP3A4 inhibition, low doses of ritonivir can reduce the metabolism of concomitantly administered protease inhibitiors, enhancing their bioavailability and efficacy.[Cayman Chemical]

使用

A selective HIV protease inhibitor

定義

ChEBI: An L-valine derivative that is an antiretroviral drug from the protease inhibitor class used to treat HIV infection and AIDS, it is often used as a fixed-dose combination with another protease inhibitor, lopinavir. Also used in combination with dasabuvir sodium hydrate, ombitasvir and paritaprevir (under the trade name Viekira Pak) for treatment of chronic hepatitis C virus genotype 1 infection as well as cirrhosis of the liver.

適応症

Although ritonavir (Norvir) is a potent inhibitor of HIV-1 and HIV-2 protease, it is not well tolerated in higher doses. It is mainly used in low doses to increase blood levels of other protease inhibitors and to extend their dosing interval. Ritonavir is more commonly associated with gastrointestinal side effects, altered taste sensation, paresthesias, and hypertriglyceridemia than are other protease inhibitors. Pancreatitis may occur in the presence or absence of hypertriglyceridemia.

brand name

Norvir (Abbott).

抗菌性

Ritonavir is active against HIV-1 and, to a lesser extent, HIV-2.

獲得抵抗性

At antiretroviral doses resistance is associated with the presence of specific amino acid substitutions in the HIV protease at positions 82 and 84. Concern about the risk for selection of ritonavir resistance when used at a subtherapeutic ‘booster’ dose has so far not been borne out by clinical experience.

一般的な説明

Ritonavir belongs to the group of protease inhibitors, which block the part of HIV called protease. Its mode of action involves binding to the protease active site and inhibiting the activity of the enzyme.

応用例(製薬)

A synthetic chemical available for oral use as soft capsules and a liquid formulation. It is now almost exclusively used as a pharmacokinetic enhancer to ‘boost’ the pharmacokinetic properties of HIV protease inhibitors in the treatment of HIV-1 infection in patients over 1 month in age.

作用機序

Because of the strong CYP450-inhibiting effects of ritonavir, the drug has found value when used in fixed-dosage combinations with other PIs to block their metabolism and act as a booster for these drugs (lopinavir/ritonavir and tipranavir/ritonavir). In these cases, ritonavir is used in a subtherapeutic dose but boosts the effectiveness of the coadministered drug. The utilization of ritonavir in a therapeutic dose for treating HIV infections appears to be decreasing, but its utilization as a booster drug is finding favor.

薬物動態学

Oral absorption: Not known/available
Cmax 600 mg twice daily: c. 11.2 mg/L
Cmin 600 mg twice daily: c. 3.7 mg/L
Plasma half-life: c. 3–5 h
Volume of distribution: c. 0.3–0.6 L/kg
Plasma protein binding: c. 97%
Absorption and distribution
Fasting and high-fat meals had no appreciable effect on oral absorption. It penetrates poorly into the CNS. The semen:plasma ratio is <0.04. It is distributed into breast milk.
Metabolism and excretion
Four oxidized metabolites have been identified, the major of which retains antiretroviral activity. Around 11% of the dose is excreted in urine, 4% as unchanged drug. The remainder is found in feces. Metabolites are eliminated primarily via the feces.
No dose adjustment is recommended in mild to moderate hepatic impairment. It should not be given to patients with severe hepatic impairment, nor should it be given as a pharmacokinetic enhancer to patients with decompensated liver disease.

臨床応用

Treatment of HIV infection in adults and children >1 month old (in combination with other antiretroviral agents)

副作用

Full (antiretroviral) doses are associated with nausea, vomiting, diarrhea and fatigue in >20% of subjects. The degree to which ritonavir at low dose is associated with specific adverse events is uncertain. In HIV-negative healthy volunteers given ‘booster’ doses of 100 mg every 12 h, the concentration of total cholesterol, low-density cholesterol and triglycerides all increased, and the concentration of high-density cholesterol concentration fell.

リトナビル 上流と下流の製品情報

原材料

準備製品


リトナビル 生産企業

Global( 430)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
Shanghai Biolang Biotechnology Co., Ltd.
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+8613397199602 Niky@biolang.cn China 587 58
Biochempartner
0086-13720134139
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15013857715
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ShenZhen Ipure Biology import and export company co.,ltd
18071025641 18071025641
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Changsha Chemoway Imp and Exp Co.,Ltd
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Hebei Senko Biotechnology Co., Ltd.
0086-133 3137 7233
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Shanghai Longyu Biotechnology Co., Ltd.
+8615821988213
+86 15821988213 info@longyupharma.com China 2500 58
Hangzhou Proserre Chemical Co.,Ltd.
+86-571-86088112
info@proserre.com China 1080 58
Capot Chemical Co.,Ltd.
+86(0)13336195806 +86-571-85586718
+86-571-85864795 sales@capotchem.com China 20012 60
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com China 22607 55

155213-67-5(リトナビル)キーワード:


  • 155213-67-5
  • 1,3-thiazol-5-ylmethyl n-[(2s,3s,5r)-3-hydroxy-5-[[(2s)-3-methyl-2-[[methyl-[(2-propan-2-yl-1,3-thiazol-4-yl)methyl]carbamoyl]amino]butanoyl]amino]-1,6-diphenyl-hexan-2-yl]carbamate
  • 1,3-THIAZOL-5-YLMETHANOL
  • CHEMBRDG-BB 4050354
  • THIAZOL-5-YL-METHANOL
  • RITONAVIR
  • RARECHEM AL BD 1261
  • 1,3-Thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[[(2S)-3-methyl-2-[[methyl-[(2-propan-2-yl-1,3-thiazol-4-yl)methyl]carbamoyl]amino]butanoyl]amino]-1,6-diphenylhexan-2-yl]carbamate
  • Ritonavir for peak identification
  • litonavir
  • 1,3-Thiazol-5-ylmethyl N-[(2s,3s,5r)-3-hydroxy-5-[[(2s)-3-methyl-2-[[methyl-[(2-propan-2-yl-1
  • Ritonavir solution
  • thiazol-5-ylMethyl ((2S,3S,5R)-3-hydroxy-5-((S)-2-(3-((2-isopropylthiazol-4-yl)Methyl)-3-Methylureido)-3-MethylbutanaMido)-1,6-diphenylhexan-2-yl)carbaMate
  • Ritonavi
  • thiazol-5-ylmethyl ((2S,3S,5S)-3-hydroxy-5-((S)-2-(3-((2-isopropylthiazol-4-yl)methyl)-3-methylureido)-3-methylbutanamido)-1,6-diphenylhexan-2-yl)carbamate
  • Ritonavir, 98%, HIV protease inhibitor
  • Ritonavir(ABT-538)
  • ABT-538
  • Liponavir Core
  • (3S,4S,6S,9S)-4-Hydroxy-12-methyl-9-(1-methylethyl)-13-[2-(1-methylethyl)-4-thiazolyl]-8,11-dioxo-3,6-bis(phenylmethyl)-2,7,10,12-tetraazatridecanoic acid, 5-thiazolylmethyl Ester
  • A 84538
  • Norvi
  • 2,4,7,12-Tetraazatridecan-13-oic acid, 10-hydroxy-2-methyl-5-(1-methylethyl)-1-[2-(1-methylethyl)-4-thiazolyl]-3,6-dioxo-8,11-bis(phenylmethyl)-, 5-thiazolylmethyl ester, (5S,8S,10S,11S)- (9CI)
  • 2,4,7,12-Tetraazatridecan-13-oic acid, 10-hydroxy-2-methyl-5-(1-methylethyl)-1-[2-(1-methylethyl)-4-thiazolyl]-3,6-dioxo-8,11-bis(phenylmethyl)-, 5-thiazolylmethyl ester, [5S-(5R*,8R*,10R*,11R*)]-
  • Abbott 84538
  • Norvir
  • NSC 693184
  • Ethinyl Estradiol, Powder
  • RITONA
  • Ritonavir Norvir
  • Ritonavir (200 mg)F0F0490.992mg/mg(ai)
  • リトナビル
  • リトナビル (JAN)
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