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Purity: ≥98%
Ritonavir (previously known as ABT-538; A-84538; RTV; ABT538, trade name: Norvir) is a potent inhibitor of HIV-1 protease and a derivative of L-valine used to treat HIV infection and AIDS. It is frequently used to improve the effectiveness of other protease inhibitors, or PIs, like lopinavir. More precisely, ritonavir is used to block CYP3A4, a specific liver enzyme that typically metabolizes protease inhibitors. Ritonavir demonstrates strong in vitro inhibitory effects against both HIV-1 and HIV-2 strains, with 50% effective concentration EC50 values of 0.022 μM and 0.16 μM, respectively.
| Targets |
CYP3A4; HIV
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| ln Vitro |
Ritonavir has a mean Ki of 19 nM, making it a very potent inhibitor of CYP3A4-mediated testosterone 6β-hydroxylation. It also has an IC50 of 4.2 μM for tolbutamide hydroxylation.[1]
Ritonavir has a mean Ki of 19 nM, making it a very potent inhibitor of CYP3A4-mediated testosterone 6β-hydroxylation. It also has an IC50 of 4.2 μM for tolbutamide hydroxylation. (Source: ) It is discovered that ritonavir is a strong inhibitor of CYP3A-mediated biotransformations (IC50 values for nifedipine oxidation and 17alpha-ethynylestradiol 2-hydroxylation are 0.07 mM, 2 mM, and 0.14 mM, respectively). The reactions mediated by CYP2D6 (IC50 = 2.5 mM) and CYP2C9/10 (IC50 = 8.0 mM) are also found to be inhibited by ritonavir.[2] In human PBMC cultures that are not infected, ritonavir increases cell viability. In uninfected human PBMC cultures, ritonavir significantly reduces caspase-3 activity, annexin V staining, and the susceptibility of PBMCs to apoptosis, which is correlated with lower levels of caspase-1 expression. In PBMCs and monocytes, ritonavir inhibits the induction of tumor necrosis factor (TNF) production in a time- and dose-dependent manner at nontoxic concentrations.[3] Ritonavir has a high affinity for p-glycoprotein as evidenced by its ability to inhibit p-glycoprotein-mediated extrusion of saquinavir, with an IC50 of 0.2 μM.[4] Ritonavir has a 13 nM Ki that potently inhibits the microsomal metabolism of ABT-378 in human liver. Inhibiting CYP3A (IC50 = 1.1 and 4.6 μM), Ritonavir in combination with ABT-378 (at 3:1 and 29:1 ratios) is less effective than Ritonavir (IC50 = 0.14 μM).[5] |
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| ln Vivo |
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| Enzyme Assay |
Ritonavir (ABT 538) is an inhibitor of testosterone 6β-hydroxylation mediated by CYP3A4, with a mean Ki of 19 nM. It also has an IC50 of 4.2 μM for tolbutamide hydroxylation. It is discovered that ritonavir (ABT 538) is a strong inhibitor of CYP3A-mediated biotransformations (IC50 values for nifedipine oxidation and 17alpha-ethynylestradiol 2-hydroxylation are 0.07 mM, 2 mM, and 0.14 mM, respectively). Inhibitors of the reactions mediated by CYP2D6 (IC50=2.5 mM) and CYP2C9/10 (IC50=8.0 mM) include ritonavir.
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| Cell Assay |
In human peripheral blood mononuclear cells that are not infected, ritonavir increases cell viability. In uninfected human PBMC cultures, ritonavir significantly lowers the susceptibility of PBMCs to apoptosis, which is correlated with lower levels of caspase-1 expression, decreases in annexin V staining, and reduces caspase-3 activity. At nontoxic concentrations, ritonavir inhibits the induction of tumor necrosis factor (TNF) production by monocytes and PBMCs in a time- and dose-dependent manner. With an IC50 of 0.2 μM, ritonavir inhibits p-glycoprotein-mediated saquinavir extrusion, suggesting a high affinity for p-glycoprotein. With a Ki of 13 nM, ritonavir potently inhibits the human liver microsomal metabolism of ABT-378. Although less potently than Ritonavir (IC50=0.14 μM), Ritonavir in combination with ABT-378 (at 3:1 and 29:1 ratios) inhibits CYP3A (IC50=1.1 and 4.6 μM).
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| Animal Protocol |
BALB/c mice
60 mg/kg i.p. |
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| References |
| Molecular Formula |
C37H48N6O5S2
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|---|---|
| Molecular Weight |
720.94
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| Exact Mass |
720.31
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| Elemental Analysis |
C, 61.64; H, 6.71; N, 11.66; O, 11.10; S, 8.90
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| CAS # |
155213-67-5
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| Related CAS # |
Ritonavir-d6;1616968-73-0;rel-Ritonavir-d6;1217720-20-1;Ritonavir metabolite;176655-55-3;Ritonavir-13C,d3
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| Appearance |
Solid powder
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| SMILES |
CC(C)C1=NC(=CS1)CN(C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC2=CC=CC=C2)C[C@@H]([C@H](CC3=CC=CC=C3)NC(=O)OCC4=CN=CS4)O
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| InChi Key |
NCDNCNXCDXHOMX-XGKFQTDJSA-N
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| InChi Code |
InChI=1S/C37H48N6O5S2/c1-24(2)33(42-36(46)43(5)20-29-22-49-35(40-29)25(3)4)34(45)39-28(16-26-12-8-6-9-13-26)18-32(44)31(17-27-14-10-7-11-15-27)41-37(47)48-21-30-19-38-23-50-30/h6-15,19,22-25,28,31-33,44H,16-18,20-21H2,1-5H3,(H,39,45)(H,41,47)(H,42,46)/t28-,31-,32-,33-/m0/s1
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| Chemical Name |
1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[[(2S)-3-methyl-2-[[methyl-[(2-propan-2-yl-1,3-thiazol-4-yl)methyl]carbamoyl]amino]butanoyl]amino]-1,6-diphenylhexan-2-yl]carbamate
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| Synonyms |
ABT-538; A 84538; Norvir; ABT538; A-84538; Norvir Sec; 538, ABT; Ritonavir; ABT 538;
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (3.47 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (3.47 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 2.5 mg/mL (3.47 mM) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Solubility in Formulation 4: 2.5 mg/mL (3.47 mM) in 5% DMSO + 95% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 5: 0.5 mg/mL (0.69 mM) in 1% DMSO 99% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 6: 30% PEG400+0.5% Tween80+5% propylene glycol: 30 mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.3871 mL | 6.9354 mL | 13.8708 mL | |
| 5 mM | 0.2774 mL | 1.3871 mL | 2.7742 mL | |
| 10 mM | 0.1387 mL | 0.6935 mL | 1.3871 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05229991 | Active Recruiting |
Drug: Lonafarnib Drug: Ritonavir |
Hepatitis D, Chronic | Soroka University Medical Center |
May 15, 2021 | Phase 3 |
| NCT05567952 | Active Recruiting |
Drug: nirmatrelvir Drug: ritonavir |
COVID-19 | Pfizer | October 19, 2022 | Phase 2 |
| NCT05438602 | Active Recruiting |
Drug: Nirmatrelvir Drug: Ritonavir |
COVID-19 | Pfizer | August 3, 2022 | Phase 2 |
| NCT03383692 | Active Recruiting |
Drug: DS-8201a Drug: Ritonavir |
Neoplasm Metastasis | Daiichi Sankyo Co., Ltd. | January 12, 2018 | Phase 2 |
| NCT03017872 | Active Recruiting |
Drug: NRTIs Drug: Ritonavir |
HIV Infections | Kirby Institute | November 23, 2017 | Phase 4 |
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