Ritonavir [155213-67-5]

Cat# T1525-500mg

Size : 500mg

Brand : TargetMol

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Ritonavir

(Synonyms: RTV, ABT 538, Abbott 84538, A 84538) Copy Product Info
Ritonavir (ABT 538) is a peptidomimetic agent that inhibits both HIV-1 and HIV-2 proteases. Ritonavir is highly inhibited by serum proteins but boosts the effect of other HIV proteases by blocking their degradation by cytochrome P450.
Ritonavir
Cas No. 155213-67-5
For research use only—not for human use. No sales to individuals. Use as intended only.
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Purity:99.96%
Color:White
COA HNMR LCMS

Product Introduction

Ritonavir AI Summary
Ritonavir demonstrates potent bioactivity against HIV-1 protease with a high binding affinity, indicated by a Ki value of 0.37 nM. It shows strong antiviral activity against HIV-1, with an effective concentration (IC90) of 150.0 nM in MT-4 cells. Its inhibitory activity extends to various mutant strains of the virus, exhibiting resistance values ranging from 2.4 to 30.0 fold, depending on the specific strain. The compound also exhibits pharmacokinetic properties with high oral bioavailability in rats, showing a maximum plasma concentration (Cmax) of 2600.0 nM and a moderate half-life of 1.2 hours. Furthermore, Ritonavir inhibits CYP3A4 enzyme activities, as demonstrated by an IC50 of 50.0 nM. Additionally, it shows inhibitory activity against ritonavir and nelfinavir-resistant HIV-1 strains, with EC50 values of 16.0 nM and 220.0 nM respectively, suggesting its potential as a promising candidate for HIV therapy..
Note: Summary generated by AI. Data source: ChEMBL
Bioactivity
Description
Ritonavir (ABT 538) is a peptidomimetic agent that inhibits both HIV-1 and HIV-2 proteases. Ritonavir is highly inhibited by serum proteins but boosts the effect of other HIV proteases by blocking their degradation by cytochrome P450.
In vivo
Ritonavir is a potent inhibitor of CYP3A-mediated biotransformation (terfenadine hydroxylation, IC50 of 0.14 mM; 17alpha-ethynylestradiol 2-hydroxylation, IC50 of 2 mM; nifedipine oxidation, IC50 of 0.07 mM).Ritonavir is a a potent inhibitor of CYP3A4-mediated testicular 6β-hydroxylation (Ki: 19 nM), and also inhibited hydroxylation by toluenesulfonylurea (IC50: 4.2 μM).Ritonavir also inhibited CYP2D6 (IC50: 2.5 mM) and CYP2C9/10 (IC50: 8.0 mM)-mediated responses.Ritonavir Ritonavir increased the cellular activity of uninfected human PBMC cultures.Ritonavir inhibited p-glycoprotein-mediated saquinavir solubilization (IC50: 0.2 μM), suggesting that Ritonavir has a high affinity for p-glycoprotein.Ritonavir significantly inhibited the metabolism of human hepatic microsomes ABT-378 (Ki: 13 nM). Ritonavir binding to ABT-378 ( in 3:1 and 29:1 ratios) was able to inhibit CYP3A (IC50: 1.1 and 4.6 μM). In cultures of uninfected human PBMCs, Ritonavir significantly reduced the susceptibility of PBMCs to apoptosis (associated with low levels of caspase-1 expression), decreased caspase-3 activity, and reduced membrane-bound protein staining. Ritonavir inhibited the induction of tumor necrosis factor produced by PBMCs and monocytes at nontoxic concentrations in a time- and dose-dependent manner.
SynonymsRTV, ABT 538, Abbott 84538, A 84538
Chemical Properties
Molecular Weight720.94
FormulaC37H48N6O5S2
Cas No.155213-67-5
SmilesCC(C)[C@H](NC(=O)N(C)CC1=CSC(=N1)C(C)C)C(=O)N[C@H](C[C@H](O)[C@H](CC1=CC=CC=C1)NC(=O)OCC1=CN=CS1)CC1=CC=CC=C1
Relative Density.1.239 g/cm3
Storage & Solubility Information
StorageStore at low temperature,Keep away from moisture Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 242.5 mg/mL (336.37 mM), Heating is recommended.
Ethanol: 7.21 mg/mL (10 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+90% Corn Oil: 2.5 mg/mL (3.47 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
Ethanol/DMSO
1mg5mg10mg50mg
1 mM1.3871 mL6.9354 mL13.8708 mL69.3539 mL
5 mM0.2774 mL1.3871 mL2.7742 mL13.8708 mL
10 mM0.1387 mL0.6935 mL1.3871 mL6.9354 mL
DMSO
1mg5mg10mg50mg
20 mM0.0694 mL0.3468 mL0.6935 mL3.4677 mL
50 mM0.0277 mL0.1387 mL0.2774 mL1.3871 mL
100 mM0.0139 mL0.0694 mL0.1387 mL0.6935 mL
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.