| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
Purity: =100%
| Targets |
Mosnodenvir blocks the NS3-NS4B interaction within the viral replication complex of dengue viruses. It is effective against all four serotypes of dengue viruses (DENV-1 through DENV-4), with the advantage of being highly potent and orally bioavailable. By inhibiting the formation of the NS3-NS4B complex, the compound disrupts viral replication at a critical step in the viral life cycle.
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| ln Vitro |
In vitro, Mosnodenvir displays picomolar to low nanomolar antiviral activity. It also inhibits SARS-CoV-2 BA.5 and XBB in Vero E6 cells with EC₅₀ values of 0.27 μM and 0.43 μM, respectively, showing broad-spectrum antiviral activity in other cell lines.
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| ln Vivo |
In vivo, in hACE2 transgenic mice, Mosnodenvir (200 mg/kg, i.p., daily × 5 days) reduced lung viral titers by >99% and alleviated lung damage, with good oral bioavailability (>80%). These results demonstrate potent in vivo efficacy against viral infection, supporting its development as a therapeutic candidate.
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| Enzyme Assay |
For non-cellular in vitro enzyme/receptor binding assays, Mosnodenvir is evaluated for its ability to inhibit the NS3-NS4B interaction. Purified NS3 and NS4B proteins or their interacting domains are used in biochemical assays such as co-immunoprecipitation, surface plasmon resonance (SPR), or fluorescence polarization to measure the compound's binding affinity and disruption of the protein-protein interaction.
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| Cell Assay |
For in vitro cellular assays, Mosnodenvir is tested in cell culture models of dengue virus infection. Susceptible cell lines (e.g., Vero E6, Huh-7) are infected with each of the four dengue virus serotypes, and treated with serial dilutions of the compound. Antiviral activity is quantified by measuring viral RNA levels, plaque reduction, or cytopathic effect inhibition to determine EC₅₀ values.
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| Animal Protocol |
For in vivo animal studies, Mosnodenvir is administered to hACE2 transgenic mice at doses such as 200 mg/kg via intraperitoneal injection daily for 5 days. Efficacy is assessed by measuring lung viral titers, evaluating lung tissue pathology, and monitoring clinical signs of infection. Oral bioavailability and pharmacokinetic parameters are also assessed in these models.
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| ADME/Pharmacokinetics |
Mosnodenvir has good oral bioavailability (>80%) in animal models. It is a highly potent, orally bioavailable compound with favorable pharmacokinetic properties suitable for once-daily dosing. The compound shows good solubility in DMSO (100 mg/mL) and can be formulated for in vivo administration using 10% DMSO + 40% PEG300 + 5% Tween80 + 45% saline.
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| Toxicity/Toxicokinetics |
Mosnodenvir is described as safe and well tolerated in preclinical studies. It has a high resistance barrier, indicating that the virus is less likely to develop resistance against this compound. Standard toxicology studies including acute and repeat-dose toxicity, genotoxicity, and safety pharmacology would be required for clinical development.
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| References |
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| Additional Infomation |
Mosnodenvir (JNJ-1802) is a pan-serotype dengue antiviral drug currently undergoing phase 2 clinical trials. It blocks viral replication by inhibiting the NS3-NS4B interaction within the viral replication complex. The compound displays picomolar to low nanomolar in vitro antiviral activity and has a high barrier to resistance. It is being developed as a therapeutic for dengue virus infections, a significant global health concern.
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| Molecular Formula |
C26H22CLF3N2O6S
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|---|---|
| Molecular Weight |
582.975895404816
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| Exact Mass |
582.083
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| CAS # |
2043343-94-6
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| PubChem CID |
122697854
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| Appearance |
White to off-white solid powder
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| LogP |
6.1
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
39
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| Complexity |
951
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| Defined Atom Stereocenter Count |
1
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| SMILES |
COC1=CC(=CC(=C1)N[C@@H](C2=C(C=C(C=C2)Cl)OC)C(=O)C3=CNC4=C3C=C(C=C4)OC(F)(F)F)S(=O)(=O)C
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| InChi Key |
QNOPDDHSGQQLCV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C26H22ClF3N2O6S/c1-36-17-9-15(10-18(11-17)39(3,34)35)32-24(19-6-4-14(27)8-23(19)37-2)25(33)21-13-31-22-7-5-16(12-20(21)22)38-26(28,29)30/h4-13,24,31-32H,1-3H3
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| Chemical Name |
2-(4-chloro-2-methoxyphenyl)-2-(3-methoxy-5-methylsulfonylanilino)-1-[5-(trifluoromethoxy)-1H-indol-3-yl]ethanone
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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) |
DMSO: 100 mg/mL (171.53 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.29 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.29 mM) (saturation unknown) 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7153 mL | 8.5766 mL | 17.1532 mL | |
| 5 mM | 0.3431 mL | 1.7153 mL | 3.4306 mL | |
| 10 mM | 0.1715 mL | 0.8577 mL | 1.7153 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.
Link: https://clinicaltrials.gov/ct2/show/NCT05201794
Conditions:DengueLink: https://clinicaltrials.gov/ct2/show/NCT05201937
Conditions:HealthyLink: https://clinicaltrials.gov/ct2/show/NCT04480736
Conditions:Healthy
Title:A Study of JNJ-64281802 in Participants With Confirmed Dengue Fever
Status:Terminated
updateDate:2024-03-01
Ctid:NCT04906980
Link: https://clinicaltrials.gov/ct2/show/NCT04906980
Conditions:DengueProducts are for research use only; We do not sell to patients
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