Ritonavir

Catalog No.S1185 Batch:S118506

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Technical Data

Formula

C37H48N6O5S2
Molecular Weight 720.94 CAS No. 155213-67-5
Solubility (25°C)* In vitro DMSO 100 mg/mL (138.7 mM)
Ethanol 100 mg/mL (138.7 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
30%PEG400 0.5%Tween80 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description 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.
Targets
CYP3A4 [1] HIV [1]
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]

Protocol (from reference)

Cell Assay:

[6]
  • Cell lines

    CD4+ T cells

  • Concentrations

    10 μM

  • Incubation Time

    36 h

  • Method

    Cells were treated with indicated concentration of drug for 36 h.
Animal Study:

[7]
  • Animal Models

    BALB/c mice

  • Dosages

    60 mg/kg

  • Administration

    i.p.

Customer Product Validation

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

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

Selleck's Ritonavir has been cited by 44 publications

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
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

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.