Uses
MMT5-14 is a remdesivir analogue with a higher antiviral activity in four variants of SARS-CoV-2 than Remdesivir.html" class="link-product" target="_blank">Remdesivir (HY-104077). MMT5-14 inhibits SARS-CoV-2, α, β, γ and δ variants with EC50s of 0.4, 2.5, 15.9, 1.7 and 5.6 μM, respectively. MMT5-14 can be used for the research of COVID-19[1].
Biological Activity
(±)-MMT5-14 is a derivative of remdesivir with antiviral activity.1 It increases the viability of Vero E6 cells infected with severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2; EC50 = 0.4 μM), as well as Vero E6 cells infected with the Alpha, Beta, Gamma, or Delta SARS-CoV-2 variants (EC50s = 2.5, 15.9, 1.7, and 5.6 μM, respectively). (±)-MMT5-14 exhibits increased plasma and lung concentrations compared with remdesivir in hamsters when administered at a dose of 10 mg/kg.
in vivo
MMT5-14 (10 mg/kg; i.v. once) shows a higher stability than remdesivir in microsomes, and shows higher concentrations of prodrugs and active metabolites (NTP) in blood and lungs[1].
| Animal Model: | Catheterized female hamsters[1] |
| Dosage: | 10 mg/kg |
| Administration: | Intravenous injection; 10 mg/kg once |
| Result: | Showed higher intact prodrugs concentration than remdesivir in lungs after 4 hours injection, increased tissue exposure in most of the tissues and showed 5- to 10-fold higher tissue selectivity in lungs compared to remdesivir. |
References
1.Hu, H., Traore, M.D.M., Li, R., et al.Optimization of the prodrug moiety of remdesivir to improve lung exposure/selectivity and enhance anti-SARS-CoV-2 activityJ. Med. Chem.65(18)12044-12054(2022)
