Ritonavir

製品コードS1185 バッチS118506

印刷

化学情報

Synonyms

ABT-538,A 84538, RTV

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₃₇H₄₈N₆O₅S₂

分子量

720.94

CAS No.

155213-67-5

Solubility (25°C)*

体外

DMSO

100 mg/mL (138.7 mM)

Ethanol

100 mg/mL (138.7 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Clear solution

30%PEG400 1 0.5%Tween80 2 5%propylene glycol

30.0mg/ml

Taking the 1 mL working solution as an example, add 300 μL of 100 mg/ml clarified PEG400 stock solution to 5 μL of Tween80, mix evenly to clarify it; add 50 μL Propylene glycol to the above system, mix evenly to clarify it; then continue to add 645 μL ddH2O to adjust the volume. to 1 mL. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Ritonavir is a Cytochrome P450 3A and Protease Inhibitor; Also inhibits Cytochrome P450 2D6, P-Glycoprotein and induces Cytochrome P450 2C19, Cytochrome P450 1A2, Cytochrome P450 2C9, Cytochrome P450 2B6 and UDP Glucuronosyltransferases. Ritonavir induces apoptosis.
in vitro	Ritonavir is a very potent inhibitor of CYP3A4 mediated testosterone 6β-hydroxylation with mean Ki of 19 nM and also inhibits tolbutamide hydroxylation with IC50 of 4.2 μM. ^[1] Ritonavir is found to be a potent inhibitor of CYP3A-mediated biotransformations (nifedipine oxidation with IC50 of 0.07 mM, 17alpha-ethynylestradiol 2-hydroxylation with IC50 of 2 mM; terfenadine hydroxylation with IC50 of 0.14 mM). Ritonavir is also found to be an inhibitor of the reactions mediated by CYP2D6 (IC50 = 2.5 mM) and CYP2C9/10 (IC50 = 8.0 mM). ^[2] Ritonavir results in an increase in cell viability in uninfected human PBMC cultures. Ritonavir markedly decreases the susceptibility of PBMCs to apoptosis correlated with lower levels of caspase-1 expression, decreases in annexin V staining, and reduces caspase-3 activity in uninfected human PBMC cultures. Ritonavir inhibits induction of tumor necrosis factor (TNF) production by PBMCs and monocytes in a time- and dose-dependent manner at nontoxic concentrations. ^[3] Ritonavir inhibits p-glycoprotein-mediated extrusion of saquinavir with an IC50 of 0.2 μM, indicating a high affinity of ritonavir for p-glycoprotein. ^[4] Ritonavir inhibits human liver microsomal metabolism of ABT-378 potently with Ki of 13 nM. Ritonavir combined with ABT-378 (at 3:1 and 29:1 ratios) inhibits CYP3A (IC50 = 1.1 and 4.6 μM), albeit less potently than Ritonavir (IC50 = 0.14 μM). ^[5]

製品説明

Ritonavir is a Cytochrome P450 3A and Protease Inhibitor; Also inhibits Cytochrome P450 2D6, P-Glycoprotein and induces Cytochrome P450 2C19, Cytochrome P450 1A2, Cytochrome P450 2C9, Cytochrome P450 2B6 and UDP Glucuronosyltransferases. Ritonavir induces apoptosis.

in vitro

Ritonavir is a very potent inhibitor of CYP3A4 mediated testosterone 6β-hydroxylation with mean Ki of 19 nM and also inhibits tolbutamide hydroxylation with IC50 of 4.2 μM. ^[1]

Ritonavir is found to be a potent inhibitor of CYP3A-mediated biotransformations (nifedipine oxidation with IC50 of 0.07 mM, 17alpha-ethynylestradiol 2-hydroxylation with IC50 of 2 mM; terfenadine hydroxylation with IC50 of 0.14 mM). Ritonavir is also found to be an inhibitor of the reactions mediated by CYP2D6 (IC50 = 2.5 mM) and CYP2C9/10 (IC50 = 8.0 mM). ^[2]

Ritonavir results in an increase in cell viability in uninfected human PBMC cultures. Ritonavir markedly decreases the susceptibility of PBMCs to apoptosis correlated with lower levels of caspase-1 expression, decreases in annexin V staining, and reduces caspase-3 activity in uninfected human PBMC cultures. Ritonavir inhibits induction of tumor necrosis factor (TNF) production by PBMCs and monocytes in a time- and dose-dependent manner at nontoxic concentrations. ^[3]

Ritonavir inhibits p-glycoprotein-mediated extrusion of saquinavir with an IC50 of 0.2 μM, indicating a high affinity of ritonavir for p-glycoprotein. ^[4]

Ritonavir inhibits human liver microsomal metabolism of ABT-378 potently with Ki of 13 nM. Ritonavir combined with ABT-378 (at 3:1 and 29:1 ratios) inhibits CYP3A (IC50 = 1.1 and 4.6 μM), albeit less potently than Ritonavir (IC50 = 0.14 μM). ^[5]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	CD4+ T cells
	濃度	10 μM
	反応時間	36 h
	実験の流れ	Cells were treated with indicated concentration of drug for 36 h.
動物実験	動物モデル	BALB/c mice
	投薬量	60 mg/kg
	投与方法	i.p.

参考

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カスタマーフィードバック

: Data from [Data independently produced by Blood, 2012, 119, 4686-97]

: Data from [Data independently produced by Blood, 2012, 119, 4686-97]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Ritonavir reverses resistance to docetaxel and cabazitaxel in prostate cancer cells with acquired resistance to docetaxel [ Cancer Drug Resist, 2024, 7:3]	PubMed: 38318527
Stabilization of the Dimeric State of SARS-CoV-2 Main Protease by GC376 and Nirmatrelvir [ Int. J. Mol. Sci, 2023, 10.3390/ijms24076062]	PubMed: None
Stabilization of the Dimeric State of SARS-CoV-2 Main Protease by GC376 and Nirmatrelvir [ Int J Mol Sci, 2023, 24(7)6062]	PubMed: 37047038
RECOVER identifies synergistic drug combinations in vitro through sequential model optimization [ Cell Rep Methods, 2023, 3(10):100599]	PubMed: 37797618
Study of the effect of biomolecules on the solubility of poorly soluble drugs [ dspace, 2023, ]	PubMed: none
The IDentif.AI-x pandemic readiness platform: Rapid prioritization of optimized COVID-19 combination therapy regimens [ NPJ Digit Med, 2022, 5(1):83]	PubMed: 35773329
Chicken heterophils extracellular traps act as early effectors against cyclopiazonic acid dependent upon NADPH oxidase, ROS and glycolysis [ Arch Toxicol, 2022, 96(7):2113-2122]	PubMed: 35508807
Combination of antiviral drugs inhibits SARS-CoV-2 polymerase and exonuclease and demonstrates COVID-19 therapeutic potential in viral cell culture [ Commun Biol, 2022, 5(1):154]	PubMed: 35194144
Reduction of CD8 T cell functionality but not inhibitory capacity by integrase inhibitors [ J Virol, 2022, JVI0173021]	PubMed: 35019724
Putative COVID-19 therapies imatinib, lopinavir, ritonavir, and ivermectin cause hair cell damage: A targeted screen in the zebrafish lateral line [ Front Cell Neurosci, 2022, 16:941031]	PubMed: 36090793

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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