Neuraminidase-IN-10

Neuraminidase-IN-10 is a potent neuraminidase (NA) inhibitor with  anti-influenza activity. Neuraminidase-IN-10 is against H1N1, H5N1, and H5N8 with IC50 values of 2.6 nM, 5.1 nM, and 1.65 nM, respectively[1].

Signaling Pathways >> Anti-infection >> Influenza Virus

Research Areas >> Infection

Neuraminidase-IN-10 displays promising anti-influenza virus activity with EC50 value of 7.28 and 0.71μM for H5N1 and H5N8, respectively in CEFs. Neuraminidase-IN-10 displays anti-influenza virus activity with EC50 values of 0.04 ± 0.04 and 28.70 ± 1.61 μM, respectively in MDCK Cells[1]. Metabolic stability is an important indicator for the assessment of drug candidates. Neuraminidase-IN-10 exhibits a T1/2 (min), CLint(mic) (μL/min/kg), CLint(liver) (mL/min/kg) and remaining (T=60 min) (%) values of 120.5 min, 11.5 μL/min/kg, 10.4 mL/min/kg and 73.8 mins, respectively[1].

Neuraminidase-IN-10 (0.156 mM-10 mM; injected into the eggs) showed good protection against both H5N1 and H5N8 strains in a dose-dependent manner in a chicken embryonated egg model [1]. Animal Model: SPF Chicken Embryonated Egg[1] Dosage: 0.156 mM; 0.625 mM; 2.5 mM; 10 mM Administration: Injected into the egg Result: were not as effective as OSC in this infection model, but also exhibited a certain therapeutic effect. The survival rates of Neuraminidase-IN-10 (H5N1: 100 and 40%, respectively; H5N8: 100 and 100%, respectively)  at 2.5 mM and 10 mM[1].

[1]. Han Ju, et al. Iterative Optimization and Structure-Activity Relationship Studies of Oseltamivir Amino Derivatives as Potent and Selective Neuraminidase Inhibitors via Targeting 150-Cavity. J Med Chem. 2022 Aug 8. doi: 10.1021/acs.jmedchem.1c01970.