MMT5-14

MMT5-14 is a remdesivir analogue with a higher antiviral activity in four variants of SARS-CoV-2 than 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].

Research Areas >> Infection

Signaling Pathways >> Anti-infection >> SARS-CoV

MMT5-14 (10 μM; 0-12 h) increases epithelial cell uptake[1]. MMT5-14 (5 μM; 2 d) shows a better in vitro antiviral activity than remdesivir[1]. Cell Viability Assay[1] Cell Line: Vero-E6 cell line Concentration: 5 μM Incubation Time: 2 days Result: Inhibited SARS-CoV-2, alpha, beta, gamma and delta variants with EC50s of 0.4, 2.5, 15.9, 1.7 and 5.6 μM, respectively.

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.

[1]. Hu H, et al. Optimization of the Prodrug Moiety of Remdesivir to Improve Lung Exposure/Selectivity and Enhance Anti-SARS-CoV-2 Activity. J Med Chem. 2022 Sep 7.