N-0385 (N 0385, Ms-Gln-Phe-Arg-kbt) is a potent, selective inhibitor of TMPRSS2 with IC50 of 1.9 nM.
N-0385 acted as a broad-spectrum coronavirus inhibitor of two SARS-CoV-2 VOCs, B.1.1.7 and B.1.351.
N-0385 is active against TMPRSS2 are potent low nanomolar inhibitors of SARS-CoV-2 in a human lung epithelial cell line (IC50=2.8 nM) and in human colonoids.
Single daily intranasal administration of N-0385 early in infection significantly improved weight loss and clinical outcomes, and yielded 100% survival in the severe K18-human ACE2 transgenic mouse model of SARS-CoV-2 disease.
TTSP-mediated proteolytic maturation of spike is critical for SARS-CoV-2 infection in vivo, N-0385 provides a novel effective early treatment option against COVID-19 and emerging SARS-CoV-2 VOCs.
Physicochemical Properties
M.Wt
644.77
Formula
C28H36N8O6S2
Appearance
Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility
10 mM in DMSO
Chemical Name/SMILES
Ms-Gln-Phe-Arg-kbt
References
1. Tirosh Shapira, et al. bioRxiv. 2021 May 4;2021.05.03.442520.
