RSV Inhibitor

Ribavirin (ICN-1229) is an antiviral agent against a broad spectrum of viruses including HCV, HIVl, and RSV. Ribavirin also has anti-orthopoxvirus and anti-variola activities.

Roflumilast (APTA-2217) is a selective PDE4 inhibitor with IC₅₀s of 0.7, 0.9, 0.7, and 0.2 nM for PDE4A1, PDE4A4, PDE4B1, and PDE4B2, respectively, without affecting PDE1, PDE2, PDE3 or PDE5 isoenzymes from various cells.

Palivizumab (MEDI 493) is a humanized monoclonal antibody against respiratory syncytial virus (RSV). Palivizumab can bind to RSV F protein with a K_d value of 1.4 nM. Palivizumab can prevent respiratory syncytial virus infection in cotton mice.

Amentoflavone (Didemethyl-ginkgetin) is a potent and orally active GABA(A) negative modulator. Amentoflavone also shows anti-inflammatory, antioxidative, anti-viral, anti-tumor, anti-radiation, anti-fungal, antibacterial activity. Amentoflavone induces apoptosis and cell cycle arrest at sub-G1 phase.

Ac-CoA Synthase-IN-1 is a potent, reversible acetate-dependent acetyl-CoA synthetase 2 (ACSS2) inhibitor with an IC₅₀ of 0.6 μM. Ac-CoA Synthase-IN-1 inhibits the respiratory syncytial virus (RSV).

2-5A (2′,5′-ApApA; 2′,5′-trioligoadenylate; 5'-O-Triphosphoryladenylyl-(2'→5')-adenylyl-(2'→5')-adenosine) TEA is a 5'-triphosphorylated (2',5') oligoadenylate. 2-5A TEA is an immunotransmitter that fuels RNase L immunity. 2-5A TEA degrades viral mRNA and inhibits protein synthesis by binding to RNase L and activating its endoribonuclease activity. 2-5A TEA can be used in RSV and cancer research.

Anti-RSV F Antibody (R4.C6) is a monoclonal antibody against RSV F, with a K_d of 0.34 nM for the post-fusion RSV F trimer. Anti-RSV F Antibody (R4.C6) recognizes a unique neutralizing epitope spanning epitopes II and IV on both pre-fusion and post-fusion RSV F. Anti-RSV F Antibody (R4.C6) can be used in studies related to respiratory syncytial virus infection.

Cyclopiazonic acid is an endoplasmic reticulum calcium ATPase (ECAs) inhibitor and human respiratory syncytial virus (RSV) inhibitor (EC₅₀ value of 4.13 μ M), which can reduce the antagonistic effect of 5-HT receptors in rat thoracic aorta, induce p53 dependent cell apoptosis and reproductive toxicity in mouse testes, and inhibit the biological activation of aflatoxin B^[1][4][5].

Ziresovir (AK0529;RO-0529) is a potent, selective, and orally bioavailable respiratory syncytial virus (RSV) fusion (F) protein (RSV F) protein inhibitor. Ziresovir shows anti-RSV activity (EC₅₀=3 nM) and highlights pharmacokinetics in animal species.

Nirsevimab (MEDI8897) is a recombinant monoclonal antibody against human respiratory syncytial virus (RSV). Nirsevimab has neutralizing activity against RSV A and RSV B viruses, with IC₅₀ values of 5.42 ng/mL and 9.71 ng/mL, respectively. Nirsevimab can be used for research on respiratory infections.

EIDD-2749 (4'-Fluorouridine) is an orally active RdRp inhibitor. EIDD-2749 effectively blocks the replication of RSV and SARS-CoV-2. EIDD-2749 also exhibits activity against HCV and lymphocytic choriomeningitis virus (LCMV). EIDD-2749 is a promising oral therapeutic candidate for COVID-19 and is also suitable for research on other RNA viruses.

Bivalirudin, a hirudin analog and anticoagulant, is a direct thrombin inhibitor. Bivalirudin inhibits thrombin-mediated fibrinogen cleavage, coagulation factor activation, and platelet activation by reversibly binding to thrombin. In addition, Bivalirudin also has certain effects of anti-virus, anti-inflammation, and vascular endothelial barrier function protection. Bivalirudin can be used for the research of thrombotic diseases and others.

Rostafuroxin (PST 2238), a digitoxigenin derivative, is an orally active and potent Na⁺,K⁺-ATPase (ATP1A1) antognist. Rostafuroxin binds specifically to the ATP1A1 extracellular domain and blocks respiratory syncytial virus (RSV)-triggered EGFR Tyr845 phosphorylation. Rostafuroxin has antihypertensive and anti-RSV activity.

GS-443902 trisodium (GS-441524 triphosphate trisodium) is a potent viral RNA-dependent RNA-polymerases (RdRp) inhibitor with IC₅₀s of 1.1 μM, 5 μM for RSV RdRp and HCV RdRp, respectively. GS-443902 trisodium is the active triphosphate metabolite of Remdesivir (GS-5734).

Verdinexor (KPT-335) is an orally active inhibitor for selective inhibitor of nuclear export (SINE). Verdinexor inhibits the respiratory syncytial virus A2 (RSV A2) replication with an IC₅₀ of 0.96 µM. Verdinexor inhibits the function of nuclear export protein Exportin 1 (XPO1/CRM1), inhibiting pro-inflammatory responses. Verdinexor exhibits antitumor effciency.

Presatovir (GS-5806) is an orally bioavailable RSV fusion inhibitor with a mean EC₅₀ value of 0.43 nM.

Clesrovimab (MK1654) is a humanized IgG1 monoclonal antibody targeting the respiratory syncytial virus (RSV) protein F. Clesrovimab binds to pre-fusion and post-fusion forms of RSV-A fusion protein with high affinity, with corresponding K_D values of 71 pM and 480 pM, respectively. Clesrovimab is applicable for the research of RSV infection.

Zelicapavir (RSV-IN-7) (example 253) is an orally active RSV inhibitor (EC₅₀: < 0.4 μΜ).

Bivalirudin TFA, a hirudin analog and anticoagulant, is a direct thrombin inhibitor. Bivalirudin TFA inhibits thrombin-mediated fibrinogen cleavage, coagulation factor activation, and platelet activation by reversibly binding to thrombin. In addition, Bivalirudin TFA also has certain effects of anti-virus, anti-inflammation, and vascular endothelial barrier function protection. Bivalirudin TFA can be used for the research of thrombotic diseases and others.

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).