Ritonavir

製品コードS1185 バッチS118504

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

3 mg/mL (4.16 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <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] This compound 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). It 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] This agent results in an increase in cell viability in uninfected human PBMC cultures. It 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. The compound inhibits induction of tumor necrosis factor (TNF) production by PBMCs and monocytes in a time- and dose-dependent manner at nontoxic concentrations. ^[3] It inhibits p-glycoprotein-mediated extrusion of saquinavir with an IC50 of 0.2 μM, indicating a high affinity of ritonavir for p-glycoprotein. ^[4] This chemical inhibits human liver microsomal metabolism of ABT-378 potently with Ki of 13 nM. When combined with ABT-378 (at 3:1 and 29:1 ratios), it 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]

This compound 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). It 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]

This agent results in an increase in cell viability in uninfected human PBMC cultures. It 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. The compound inhibits induction of tumor necrosis factor (TNF) production by PBMCs and monocytes in a time- and dose-dependent manner at nontoxic concentrations. ^[3]

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

This chemical inhibits human liver microsomal metabolism of ABT-378 potently with Ki of 13 nM. When combined with ABT-378 (at 3:1 and 29:1 ratios), it 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 this compound 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

https://pubmed.ncbi.nlm.nih.gov/9278209/
https://pubmed.ncbi.nlm.nih.gov/8613951/
https://pubmed.ncbi.nlm.nih.gov/10551732/

https://pubmed.ncbi.nlm.nih.gov/11230802/
https://pubmed.ncbi.nlm.nih.gov/10421617/
https://pubmed.ncbi.nlm.nih.gov/29686423/
https://pubmed.ncbi.nlm.nih.gov/33722611/

+ 展开

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：

Neospora caninum triggers the release of heterophil extracellular traps in chickens [ Vet Parasitol, 2025, 337:110471]	PubMed: 40245810
Enhancer reprogramming underlies therapeutic utility of a SMARCA2 degrader in SMARCA4 mutant cancer [ Cell Chem Biol, 2024, S2451-9456(24)00396-9]	PubMed: 39378885
The host-targeted antiviral drug Zapnometinib exhibits a high barrier to the development of SARS-CoV-2 resistance [ Antiviral Res, 2024, 225:105840]	PubMed: 38438015
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

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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