Cap-dependent endonuclease-IN-26

Cap-dependent endonuclease-IN-26 is a cap-dependent endonuclease (CEN) inhibitor with an IC50 of 286 nM. Cap-dependent endonuclease-IN-26 shows antiviral activity against many influenza A and B strains[1].

Signaling Pathways >> Anti-infection >> Influenza Virus

Research Areas >> Infection

Cap-dependent endonuclease-IN-26 (compound 2v) exhibits broad antiviral spectrum. Cap-dependent endonuclease-IN-26 shows antiviral activity against the H1N1 type, including the reverse genetic strain (rgA/WSN/33), oseltamivir-resistant strain (rgA/WSN/33-NA/H274Y), clinically isolated strain (A/PR/8/34), H3N2 A/Victoria/3/75, H3N2 A/HongKong/8/68, influenza B/Hong Kong/5/72, and influenza B/Maryland/1/59 with EC50 values 165.1 nM, 80.4 nM, 183.0 nM, 828.8 nM, 301.5 nM, 124.3 nM, and 176.0 nM, respectively[1].

In rats, Cap-dependent endonuclease-IN-26 (compound 2v) exhibits reasonable in vivo clearance with 10.9 mL/min/kg[1]. In a mouse influenza B (B/Maryland/1/59) model, Cap-dependent endonuclease-IN-26 (compound 2v; intravenous administration; 0.08-10 mg/kg; q.d.;1 day) shows dose-dependent efficacy in an immediate treatment model[1].

[1]. Masayoshi Miyagawa, et al. Synthesis and SAR Study of Carbamoyl Pyridone Bicycle Derivatives as Potent Inhibitors of Influenza Cap-dependent Endonuclease. J Med Chem. 2019 Sep 12;62(17):8101-8114.