| Field | Specification |
|---|---|
| Target | |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C28H25F5N4O4 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
JNJ-8003 is a potent, orally active, non-nucleoside inhibitor of RSV polymerase, with an IC50 of 0.29 nM. It targets the L protein polymerase complex of RSV (IC50 = 0.67 nM), blocking transcription and replication of the viral genome by inhibiting RNA-dependent RNA polymerase (RdRp) activity. The compound shows subnanomolar activity in vitro and notable efficacy in mouse and neonatal lamb models, and can be used to study respiratory syncytial virus (RSV)[1][2]. It is supplied as an off-white to light yellow solid (C28H25F5N4O4, MW 576.51) at 99.84% purity.
Physical & Chemical Properties
| CAS Number | 3118087-68-3 |
|---|---|
| Molecular Formula | C28H25F5N4O4 |
| Molecular Weight | 576.51 g/mol |
| Purity | 99.84% |
| Appearance | Solid |
| Color | Off-white to light yellow |
| 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 |
| Target | RNA Polymerase |
| Signaling Pathway | Anti-infection; Cell Cycle/DNA Damage |
| Solubility | In Vitro: DMSO: 125 mg/mL (216.82 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | Powder: -20°C, 3 years. In solvent: -80°C, 6 months; -20°C, 1 month. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 125 mg/mL (216.82 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); avoid repeated freeze-thaw cycles.
Data provided by the manufacturer.
In Vitro
At the initiation and early elongation stages, JNJ-8003 (5 μM) inhibits RVS RNA replication and transcription[1]. At the cellular level (HeLa cells), JNJ-8003 shows significant anti-RSV activity with an EC50 of 0.82 nM, and is cytotoxic to Hela cells with a CC50 of 27.7 μM[2].
In Vivo
Outstanding efficacy in RSV mouse and neonatal lamb models is shown by JNJ-8003 (0.25-100 mg/kg, p.o., once daily for 4-5 days)[2].
| Animal Model | RSV-A2 infection model established in 6-8 week old female BALB/c mice (Janvier)[2] |
|---|---|
| Dosage | 1, 4, 10, 40, 100 mg/kg |
| Administration | Oral administration (p.o.), once daily for 4 days |
| Result | Dose-dependently inhibited virus, with viral titers dropping below the detection limit at doses of 10 mg/kg and above. |
| Animal Model | RSV M37 infection model established in lamb (from LambCure)[2] |
|---|---|
| Dosage | 0.25, 1, 4 mg/kg |
| Administration | Oral administration (p.o.), once daily for 5 days |
| 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). |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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