WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 555848
Description: GRP-60367 is a potent and selective rabies virus (RABV) entry inhibitor with nanomolar potency against some RABV strains. GRP-60367 inhibits entry of a subset of RABV strains. Resistance profiling of the chemotype revealed hot spots in conserved hydrophobic positions of the RABV G protein fusion loop that were confirmed in transient cell-to-cell fusion assays. Transfer of RABV G genes with signature resistance mutations into a recombinant VSV backbone resulted in the recovery of replication-competent virions with low susceptibility to the inhibitor.
MedKoo Cat#: 555848
Chemical Formula: C21H27N3O2
Exact Mass: 353.2103
Molecular Weight: 353.466
Elemental Analysis: C, 71.36; H, 7.70; N, 11.89; O, 9.05
Synonym: GRP-60367; GRP 60367; GRP60367;
IUPAC/Chemical Name: (4-((2-(2,5-dimethylphenoxy)ethyl)amino)piperidin-1-yl)(pyridin-4-yl)methanone
InChi Key: WNJMKSOJWRDLLM-UHFFFAOYSA-N
InChi Code: InChI=1S/C21H27N3O2/c1-16-3-4-17(2)20(15-16)26-14-11-23-19-7-12-24(13-8-19)21(25)18-5-9-22-10-6-18/h3-6,9-10,15,19,23H,7-8,11-14H2,1-2H3
SMILES Code: O=C(N1CCC(NCCOC2=CC(C)=CC=C2C)CC1)C3=CC=NC=C3
Rabies virus (RABV) causes a severe and fatal neurological disease, but morbidity is vaccine preventable and treatable prior to the onset of clinical symptoms. However, immunoglobulin (IgG)-based rabies postexposure prophylaxis (PEP) is expensive, restricting access to life-saving treatment, especially for patients in low-income countries where the clinical need is greatest, and does not confer cross-protection against newly emerging phylogroup II lyssaviruses.
Du Pont V, Wirblich C, Yoon JJ, Cox RM, Schnell MJ, Plemper RK. Identification and Characterization of a Small-Molecule Rabies Virus Entry Inhibitor. J Virol. 2020 Jun 16;94(13):e00321-20. doi: 10.1128/JVI.00321-20. PMID: 32321812; PMCID: PMC7307179.