rsv polymerase

BTA-9881 is a novel RSV fusion inhibitor with oral activity and antiviral activity for the study of respiratory syncytial virus infections.

Totrombopag (SB559448) is a candidate compound for action on RSV polymerase.

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

JNJ-7184 is a non-nucleoside inhibitor of the RSV-Large (L) polymerase, with pEC50 and pCC50 values of 7.86 and 4.29, respectively, in Hela cells. It inhibits the initiation or early elongation phases, thereby preventing RSV replication and transcription.

RSV L-protein-IN-4 (Compound C) is a noncompetitive inhibitor of the RSV polymerase, exhibiting an IC50 of 0.88 μM and demonstrating potent antiviral activity against RSV strains with an EC50 of 0.25 μM [1].

ALS-8112 (ALS 008112) is a selective and potent inhibitor of respiratory syncytial virus (RSV) polymerase with an IC50 value of 0.02 μM. ALS-8112 exhibits antiviral activity and inhibits the RNA polymerase activity of the RSV L-P protein complex through RNA chain termination. virus infections.

PC786 is a potent and selective non-nucleoside RSV L-protein polymerase inhibitor for inhalation therapy of RSV infections, with antiviral activity against RSV-A (IC50=0.09-0.71 nM) and RSV-B (IC 50=1.3-50.6 nM), and the ability to inhibit RSV RNA-dependent RNA polymerase in HEp-2 cells ( RdRp).

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].

GHP-88309 is an orally active, broad-spectrum anti-paramyxovirus agent that targets viral polymerase, interrupting viral RNA synthesis. It effectively inhibits respiratory syncytial virus (RSV), measles virus (MeV), and canine distemper virus (CDV) with an EC50 of 0.06-1.2 μM. In mouse models, GHP-88309 demonstrates significant anti-infective activity.

Lumicitabine (ALS-008176) is an RSV polymerase inhibitor.

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 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].

JNJ-8003 is a potent inhibitor of RSV Polymerase, impeding early RNA transcription and replication by inhibiting nucleotide polymerization [1].

AVG-233 is an orally available RNA-dependent RNA polymerase (RdRp) inhibitor with antiviral activity that blocks respiratory syncytial virus and SARS-CoV-2 replication.AVG-233 is used in the study of respiratory syncytial virus infections.

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].