rsv-in-2

RSV-IN-2 is a powerful compound that acts as a dual inhibitor of both wild-type and mutant respiratory syncytial virus (RSV) fusion proteins. It efficiently inhibits the activity of these proteins, with an EC50 value of 0.27 nM for the wild-type and 0.70 nM for the D486N-mutant protein.

RSV IAV-IN-2 (compound 14c) is a potent dual inhibitor of RSV IAV, demonstrating lower cytotoxicity than the clinical drug Ribavirin, and shows potential for RSV and or IAV infection research [1].

RSV L-protein-IN-2 (Compound A) is a noncompetitive inhibitor of the RSV polymerase with an IC50 of 4.5 μM and demonstrates antiviral activity against long RSV strains with an EC50 of 1.3 μM [1].

Ganglioside GM1 asialo is a component of cellular lipid rafts and can be formed by the cleavage of the sialic acid residue from ganglioside GM1 by neuraminidase. Ganglioside GM1 asialo is a glycolipid receptor for P. aeruginosa flagellin and stimulates defensive responses in host cells, including extracellular ATP release, calcium mobilization, and ERK1/2 phosphorylation when stimulated by flagellin and an anti-ganglioside GM1 asialo antibody. The percentage of ganglioside GM1 asialo-positive natural killer (NK) and CD8+ T cells in lung is increased in a mouse model of respiratory syncytial virus (RSV) infection compared with healthy animals. Depletion of ganglioside GM1 asialo-positive NK and T cells reduces IFN-γ levels in the lung, reduces weight loss, and increases lung viral load in RSV-infected mice. Ganglioside GM1 asialo mixture contains ganglioside GM1 asialo molecular species with C18:1 and C20:1 sphingoid backbones.

GS-441524tris-isobutyryl ester is a prodrug form of the antiviral nucleoside analog and remdesivir metabolite GS-441524 .1It reduces the cytopathic effect of respiratory syncytial virus (RSV) in infected HEp-2 cells with an EC50value of 0.26 μM. 1.Mackman, R.L., Hui, H.C., Perron, M., et al.Prodrugs of a 1’-CN-4-aza-7,9-dideazaadenosine C-nucleoside leading to the discovery of remdesivir (GS-5734) as a potent inhibitor of respiratory syncytial virus with efficacy in the african green monkey model of RSVJ. Med. Chem.64(8)5001-5017(2021)

RSV L-protein-IN-3 is an inhibitor of wild-type RSV polymerase with an IC50 of 10.4 μM and an EC50 of 2.1 μM (against RSV) and exhibits lower cytotoxicity than the clinical agent Ribavirin [1].

RSV L-protein-IN-5 (Compound E) serves as a potent inhibitor of the Respiratory Syncytial Virus (RSV), with an EC50 value of 0.1 μM. It targets RSV polymerase with an IC50 of 0.66 μM and impedes RSV mRNA synthesis through the inhibition of transcript guanylation. The compound demonstrates moderate cytotoxicity, with a CC50 of 10.7 μM in HEp-2 cells, and effectively reduces viral titers in mouse models of RSV infection [1].

Ribavirin-13C5is intended for use as an internal standard for the quantification of ribavirin by GC- or LC-MS. Ribavirin is an antiviral guanosine nucleoside analog.1,2Upon entry into cells, ribavirin is metabolized to an active triphosphate form that induces viral RNA chain termination and inhibits viral polymerases. It reduces replication in a panel of seven RNA and four DNA viruses in Vero cells (EC50s = 2-95 μg/ml).3Ribavirin also reduces replication of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) in Vero cells (EC50= 109.5 μM).4Aerosol administration of ribavirin (30 mg/kg) reduces mortality in a mouse model of influenza A infection.5Formulations containing ribavirin have been used in the treatment of respiratory syncytial virus (RSV), hepatitis C virus (HCV), and viral hemorrhagic fevers. 1.Gilbert, B.E., and Knight, V.Biochemistry and clinical applications of ribavirinAntimicrob. Agents Chemother.30(2)201-205(1986) 2.Gordon, C.J., Tchesnokov, E.P., Woolner, E., et al.Remdesivir is a direct-acting antiviral that inhibits RNA-dependent RNA polymerase from severe acute respiratory syndrome coronavirus 2 with high potencyJ. Biol. Chem.295(20)6785-6797(2020) 3.Kirsi, J.J., North, J.A., McKernan, P.A., et al.Broad-spectrum antiviral activity of 2-β-D-ribofuranosylselenazole-4-carboxamide, a new antiviral agentAntimicrob. Agents Chemother.24(3)353-361(1983) 4.Wang, M., Cao, R., Zhang, L., et al.Remdesivir and chloroquine effectively inhibit the recently emerged novel coronavirus (2019-nCoV) in vitroCell Res.30(3)269-271(2020) 5.Wilson, S.Z., Knight, V., Wyde, P.R., et al.Amantadine and ribavirin aerosol treatment of influenza A and B infection in miceAntimicrob. Agents Chemother.17(4)642-648(1980)

RSV-IN-4 (Compound 2) is a dual inhibitor of respiratory syncytial virus (RSV) and influenza virus A (IAV), demonstrating anti-RSV activity with an EC50 of 11.76 μM.

Ribavirin (Tribavirin) is a synthetic nucleoside analog of ribofuranose with activity against hepatitis C virus and other RNA viruses.