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.

Lonafarnib (Sch66336) is an orally active, blood-brain barrier penetrant farnesyltransferase (FPTase) inhibitor. Lonafarnib increases the phosphorylation levels of Akt, CaMKII and CREB, upregulates BDNF expression in the hippocampus, elevates the content of α7nAChR on cell membranes, and blocks the isoprenylation of H-Ras. Lonafarnib repairs synapses and reverses spatial memory deficits in Aβ1-42 model mice. Lonafarnib inhibits RSV fusion and replication, and alleviates virus-induced lung injury. Lonafarnib activates the lysosomal and autophagic pathways, and reduces the phosphorylation and aggregation of tau. Lonafarnib acts synergistically with Sorafenib (HY-10201) to promote apoptosis, and inhibits the proliferation and invasion of melanoma cells. Lonafarnib inhibits the farnesylation of progerin, repairs nuclear membrane defects, and activates the cGAS-STING-STAT1 signaling pathway. Lonafarnib can be used in research related to diseases including Alzheimer's disease, viral infections, melanoma, and progeria.

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.

4'-C-Azido-2'-deoxy-2'-fluorocytidine is an antiviral agent. 4'-C-Azido-2'-deoxy-2'-fluorocytidine potently inhibits RNA synthesis of crude RSV RNP complexes with an IC₅₀ of 0.1 μM. 4'-C-Azido-2'-deoxy-2'-fluorocytidine inhibits RSV replication in a subgenomic RSV replicon system. 4'-C-Azido-2'-deoxy-2'-fluorocytidine can be used for the research of respiratory syncytial virus (RSV) infection.

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.

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).

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.