JNJ-8003
Based on 1 Customer Validation
JNJ-8003 is a potent and orally active non-nucleoside RSV polymerase inhibitor with an IC50 of 0.29 nM. JNJ-8003 targets the L protein polymerase complex of RSV (IC50 = 0.67 nM), and blocks the transcription and replication of the viral genome by inhibiting the activity of RNA-dependent RNA polymerase (RdRp). JNJ-8003 displays subnanomolar activity in vitro as well as prominent efficacy in mice and a neonatal lamb models. JNJ-8003 can be used for the study of respiratory syncytial virus (RSV).
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- Pureté: 99.84%
- CAS No.: 3118087-68-3
- Formule: C28H25F5N4O4
- Masse moléculaire:576.51
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Stockage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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RNA Polymerase |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | CC50 |
27.7 μM
Compound: 28; JNJ-8003
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Cytotoxicity against human HeLa cells measured after 3 days by ATPlite kit assay
Cytotoxicity against human HeLa cells measured after 3 days by ATPlite kit assay
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[PMID: 39105710] |
JNJ-8003 (5 μM) inhibits RVS RNA replication and transcription at the initiation and early elongation stage[1].
JNJ-8003 exhibits significant anti-RSV activity at the cellular level (HeLa cells) with an EC50 of 0.82 nM and shows cytotoxicity against Hela cells with a CC50 of 27.7 μM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | CL | T1/2 | Vdss | Cmax | AUC0-last | F |
|---|---|---|---|---|---|---|---|---|
| Dog[1] | 0.5 mg/kg | i.v. | 5.62 mL/min/kg | 4.25 h | 1.49 L/kg | / | / | / |
| Dog[1] | 0.5 mg/kg | p.o. | / | / | / | 249 ng/mL | 1200 ng·h/mL | 81 % |
| Mice[1] | 10 mg/kg | p.o. | / | / | / | 1727 ng/mL | 9578 ng·h/mL | 61 % |
| Mice[1] | 2.5 mg/kg | i.v. | 10.6 mL/min/kg | 1.95 h | 1.68 L/kg | / | / | / |
| Rat[1] | 1.25 mg/kg | i.v. | 8.03 mL/min/kg | 3.15 h | 1.04 L/kg | / | / | / |
| Rat[1] | 5 mg/kg | p.o. | / | / | / | 401 ng/mL | 2097 ng·h/mL | 20 % |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:RSV-A2 infection model established in 6-8 week old female BALB/c mice (Janvier)[2]
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Dosage:1, 4, 10, 40, 100 mg/kg
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Administration:Oral administration (p.o.), once daily for 4 days
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Result:Dose-dependently inhibited virus, with viral titers dropping below the detection limit at doses of 10 mg/kg and above.
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Animal Model:RSV M37 infection model established in lamb (from LambCure)[2]
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Dosage:0.25, 1, 4 mg/kg
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Administration:Oral administration (p.o.), once daily for 5 days
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Result:Decreased the lung virus titer below the detection limit at 4 mg/kg.
Completed resolution of lung inflammation and lesions (H&E scores returned to normal).
Chemical Information
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CAS No. 3118087-68-3
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Appearance Solid
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Masse moléculaire 576.51
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Formule C28H25F5N4O4
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Color Off-white to light yellow
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SMILES
CC(N=N1)=CC2=C1C(OC)=CC(C(NC[C@](C(F)(F)F)(O)C3=CC(C(C)(C)O)=C(F)C(C4=CC=C(F)C=C4)=N3)=O)=C2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 125 mg/mL (216.82 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (277 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Yu X, et al. Structural and mechanistic insights into the inhibition of respiratory syncytial virus polymerase by a non-nucleoside inhibitor. Commun Biol. 2023 Oct 21;6(1):1074. [Content Brief]
[2]. Grosse S, et al. Discovery of gem-Dimethyl-hydroxymethylpyridine Derivatives as Potent Non-nucleoside RSV Polymerase Inhibitors. J Med Chem. 2024 Aug 22;67(16):13723-13736. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7346 mL | 8.6729 mL | 17.3458 mL | 43.3644 mL |
| 5 mM | 0.3469 mL | 1.7346 mL | 3.4692 mL | 8.6729 mL | |
| 10 mM | 0.1735 mL | 0.8673 mL | 1.7346 mL | 4.3364 mL | |
| 15 mM | 0.1156 mL | 0.5782 mL | 1.1564 mL | 2.8910 mL | |
| 20 mM | 0.0867 mL | 0.4336 mL | 0.8673 mL | 2.1682 mL | |
| 25 mM | 0.0694 mL | 0.3469 mL | 0.6938 mL | 1.7346 mL | |
| 30 mM | 0.0578 mL | 0.2891 mL | 0.5782 mL | 1.4455 mL | |
| 40 mM | 0.0434 mL | 0.2168 mL | 0.4336 mL | 1.0841 mL | |
| 50 mM | 0.0347 mL | 0.1735 mL | 0.3469 mL | 0.8673 mL | |
| 60 mM | 0.0289 mL | 0.1445 mL | 0.2891 mL | 0.7227 mL | |
| 80 mM | 0.0217 mL | 0.1084 mL | 0.2168 mL | 0.5421 mL | |
| 100 mM | 0.0173 mL | 0.0867 mL | 0.1735 mL | 0.4336 mL |
JNJ-8003 Related Classifications
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