Home Proteases HIV Protease inhibitor - P450 (e.g. CYP17) inhibitor - COVID-19 inhibitor - Apoptosis related activator Ritonavir For research use only.

Ritonavir

Synonyms: ABT-538,A 84538, RTV

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.

Ritonavir Chemical Structure

Ritonavir Chemical Structure

CAS: 155213-67-5

Selleck's Ritonavir has been cited by 42 publications

Purity & Quality Control

Batch: Purity: 99.98%
99.98

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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
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]
Cell Research Cell lines CD4+ T cells
Concentrations 10 μM
Incubation Time 36 h
Method

Cells were treated with indicated concentration of drug for 36 h.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06139796 Not yet recruiting HIV Infections PENTA Foundation|AMS-PHPT Research Collaboration|Institut National de la Santé Et de la Recherche Médicale France|Centre Mère et Enfant de la Fondation Chantal Biya|Centre Hospitalier National d''Enfants Albert Royer|University of Zimbabwe Clinical Research Centre (UZCRC)|Baylor College of Medicine June 2024 Phase 1|Phase 2
NCT05953545 Not yet recruiting Chronic Hepatitis Delta National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)|National Institutes of Health Clinical Center (CC) January 12 2024 Phase 2
NCT06016556 Recruiting Covid-19 Pfizer October 17 2023 --
NCT06085924 Not yet recruiting COVID-19 Pfizer October 23 2023 --
NCT05718518 Recruiting Healthy|COVID-19 Ascletis Pharmaceuticals Co. Ltd. January 13 2023 Phase 1
NCT05749445 Recruiting Hospitalized Patients First People''s Hospital of Hangzhou|Hangzhou Cancer Hospital|First People''s Hospital of Lin''an District|First People''s Hospital of Yuhang District December 15 2022 --

Chemical lnformation & Solubility

Molecular Weight 720.94 Formula

C37H48N6O5S2
CAS No. 155213-67-5 SDF Download Ritonavir SDF
Smiles CC(C)C(NC(=O)N(C)CC1=CSC(=N1)C(C)C)C(=O)NC(CC(O)C(CC2=CC=CC=C2)NC(=O)OCC3=CN=CS3)CC4=CC=CC=C4
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (138.7 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble


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In vivo
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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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