RSV-IN-14
RSV-IN-14 is an orally active pre-fusion F protein inhibitor of respiratory syncytial virus (RSV), with a Kd of 5.0 μM, and exhibits lung-targeted distribution properties. RSV-IN-14 binds to the central cavity of the trimeric pre-fusion F protein, locks it in the pre-fusion state, and inhibits the conformational changes required for membrane fusion to block viral entry. RSV-IN-14 suppresses respiratory syncytial virus-induced syncytium formation. RSV-IN-14 can be used in studies on respiratory syncytial virus infection.
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- CAS. Nr.: 3103996-88-6
- Formel: C22H29N5O3S
- Molecular Weight:443.56
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Help & FAQs
Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
RSV pre-fusion F protein 5.0 μM (Kd) |
In Vitro
RSV-IN-14 (compound 7d) demonstrates highly potent anti-RSV activity against the RSV-long strain and minimal cytotoxicity in HEp-2 cells, with an EC50 of 3.65 nM[1].
RSV-IN-14 (50 μM) exerts potent broad-spectrum inhibitory activity against diverse clinically isolated RSV subtype strains in in vitro[1].
RSV-IN-14 forms a stable protein-ligand complex by directly binding to the prefusion conformational epitope of the RSV F protein[1].
RSV-IN-14 (0.1-1.0 nM) effectively suppresses RSV infection, viral protein expression, and syncytium formation while restoring normal epithelial structure in aged human nasal organoids[1].
RSV-IN-14 is classified as a medium-permeability compound with good cellular uptake potential[1].
RSV-IN-14 exhibits low cardiac toxicity risk as indicated by its relatively high hERG IC50 value[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
In Vivo
RSV-IN-14 (12.5-50 mg/kg; p.o.; twice daily; 3 consecutive days) effectively inhibits pulmonary RSV replication and ameliorates RSV-induced severe lung injury in 65-week-old aged C57BL/6 mice, with the 50 mg/kg dose achieving 82% reduction in both viral titer and RSV-F gene copies[1].
RSV-IN-14 (12.5-100 mg/kg; p.o.; twice daily; 3 consecutive days) reduces RSV viral loads by over 90% and mitigates virus-induced pulmonary inflammation and tissue injury in 4-week-old juvenile C57BL/6 mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c mice (4-week-old female)[1]
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Dosage:100 mg/kg
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Administration:p.o.; twice daily; 3 consecutive days
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Result:Attenuated RSV-induced progressive body weight loss in infected mice.
Reduced the elevated lung index by 12.9% relative to the RSV-infected control group at 3 days post-infection.
Reduced pulmonary RSV-F protein mRNA expression by 92.98% at 3 days post-infection.
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Animal Model:C57BL/6 mice (4-week-old female)[1]
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Dosage:12.5 mg/kg; 50 mg/kg; 100 mg/kg
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Administration:p.o.; twice daily; 3 consecutive days
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Result:Produced greater than 90% reduction in RSV-F gene copy levels in lung tissue across all tested doses.
Resulted in only transient initial body weight decrease at 1 day post-infection followed by recovery over subsequent 2 days, in contrast to the 18.8% progressive body weight loss observed in untreated RSV-infected mice by 3 days post-infection.
Reduced lung index values, attenuated inflammatory cell infiltration and virus-induced lung tissue damage, and markedly suppressed pulmonary mRNA expression of the pro-inflammatory cytokines TNF-α, IL-1β, and IL-6 across all dose groups.
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Animal Model:C57BL/6 mice (65-week-old male)[1]
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Dosage:12.5 mg/kg; 50 mg/kg
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Administration:p.o.; twice daily; 3 consecutive days
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Result:Alleviated the downward trend of body weight in RSV-infected aged mice, though body weight recovery was slower than that observed in juvenile mice.
Produced an 82% reduction in lung viral titer and an 82% reduction in RSV-F gene copies at the 50 mg/kg dose level.
Reduced the elevated lung index values by 18-32% relative to RSV-infected mice.
Alleviated the severe RSV-induced lung pathology including lymphocytic/granulocytic infiltration, alveolar septal thickening, necrotic cellular debris, alveolar/bronchial hemorrhage, perivascular lymphocytic cuffing and vascular congestion, with the 50 mg/kg dose demonstrating greater efficacy than 12.5 mg/kg.
Chemical Information
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CAS. Nr. 3103996-88-6
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Molecular Weight 443.56
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Formel C22H29N5O3S
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SMILES
O=S1(CCN(C2=NC(NCC3(N)COC3)=C(CC(C)CC4)C4=N2)CC5=C1C=CC=C5)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
RSV-IN-14 Related Classifications
HY-189244 Related Classifications
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