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| Targets |
JNJ-2408068 targets respiratory syncytial virus (RSV). It is a small-molecule inhibitor that exhibits potent antiviral activity against RSV. The compound significantly inhibits the replication of RSV subtypes A and B. Its mechanism of action involves inhibition of viral replication, though the specific molecular target has not been fully elucidated in the available literature.
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| ln Vitro |
In vitro, JNJ-2408068 exhibits potent antiviral activity against RSV with EC50 values of 1.4 and 2.1 nM. Its activity is typically assessed in cell-based antiviral assays using RSV-infected cell lines. The compound's ability to inhibit viral replication is measured by quantifying viral RNA or protein levels, or by measuring the reduction in cytopathic effect.
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| ln Vivo |
In vivo, JNJ-2408068 significantly inhibits replication of RSV A and B subtypes in the lungs of cotton rats without any evidence of toxicity. This demonstrates its potential as an antiviral agent for the treatment of RSV infection. The compound's efficacy in the cotton rat model supports its utility for studying RSV pathogenesis and therapeutic intervention.
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| Enzyme Assay |
As an antiviral compound, JNJ-2408068 is not typically evaluated in cell-free receptor binding assays. Its activity is assessed in cell-based antiviral assays measuring inhibition of viral replication. The compound's mechanism of action can be studied using time-of-addition assays, resistance selection, and other virological methods.
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| Cell Assay |
In vitro cell-based experiments with JNJ-2408068 typically involve RSV-infected cell lines such as HEp-2 or A549 cells. Cells are infected with RSV and treated with various concentrations of the compound. Viral replication is assessed by measuring the production of viral proteins (e.g., by immunofluorescence or ELISA) or by quantifying viral RNA using qRT-PCR. The EC50 is determined from concentration-response curves.
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| Animal Protocol |
In vivo animal experiments with JNJ-2408068 have been conducted in cotton rats. In typical protocols, cotton rats are infected intranasally with RSV and then treated with the compound via various routes of administration. At the end of the study, lungs are harvested, and viral titers are measured by plaque assay or qRT-PCR. Histological analysis is performed to assess lung pathology and toxicity.
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| ADME/Pharmacokinetics |
No detailed pharmacokinetic data is publicly available for JNJ-2408068. As an antiviral compound, its absorption, distribution, metabolism, and excretion (ADME) properties would be expected to support its efficacy in the lungs. Its half-life and bioavailability have not been extensively characterized.
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| Toxicity/Toxicokinetics |
In preclinical studies, JNJ-2408068 significantly inhibited RSV replication in cotton rat lungs without any evidence of toxicity. This suggests a favorable safety profile at therapeutic doses. The compound is for research use only and is not intended for human therapeutic applications.
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| References |
: Cold virus fusion or stopping fusion cold--inhibitors of the human respiratory syncytial virus F protein. Recent Pat Antiinfect Drug Discov. 2006 Jun;1(2):247-54.
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| Additional Infomation |
JNJ-2408068 has a CAS number of 317846-22-3. It is also known as HE066500 and R170591. The compound is a potent RSV inhibitor with EC50 values of 1.4 and 2.1 nM. It significantly inhibits replication of RSV A and B subtypes in cotton rat lungs without toxicity. It is available for research purposes only.
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| Molecular Formula |
C22H30N6O
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|---|---|
| Molecular Weight |
394.5132
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| Exact Mass |
394.248
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| CAS # |
317846-22-3
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| Related CAS # |
317846-22-3;317846-21-2 (4HCl);
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| PubChem CID |
511013
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| Appearance |
White to off-white solid powder
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| LogP |
2.697
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
29
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| Complexity |
514
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| Defined Atom Stereocenter Count |
0
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| SMILES |
OC1=CC=C(C)N=C1CN2C3=CC=CC(C)=C3N=C2NC4CCN(CCN)CC4
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| InChi Key |
RDQSNNMSDOHAPG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H30N6O/c1-15-4-3-5-19-21(15)26-22(25-17-8-11-27(12-9-17)13-10-23)28(19)14-18-20(29)7-6-16(2)24-18/h3-7,17,29H,8-14,23H2,1-2H3,(H,25,26)
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| Chemical Name |
2-[[2-[[1-(2-aminoethyl)piperidin-4-yl]amino]-4-methylbenzimidazol-1-yl]methyl]-6-methylpyridin-3-ol
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| Synonyms |
HE 066500 JNJ-2408068R170591 R 170591 HE066500 R-170591HE-066500 JNJ 2408068 JNJ2408068.
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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 (~253.5 mM; with ultrasonication)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (6.34 mM) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication and warming and heat to 60°C.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and 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 (6.34 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication and warming and heat to 60°C. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. 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 3: ≥ 2.5 mg/mL (6.34 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 DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5348 mL | 12.6739 mL | 25.3479 mL | |
| 5 mM | 0.5070 mL | 2.5348 mL | 5.0696 mL | |
| 10 mM | 0.2535 mL | 1.2674 mL | 2.5348 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.
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