Name | GRP-60367 |
Synonyms | GRP-60367 (4-((2-(2,5-Dimethylphenoxy)ethyl)amino)piperidin-1-yl)(pyridin-4-yl)methanone |
CAS | 1309241-34-6 |
Molecular Formula | C21H27N3O2 |
Molar Mass | 353.46 |
Solubility | Soluble in DMSO |
Storage Condition | -20℃ |
Use | 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. |
In vitro study | GRP-60367 inhibits entry of a subset of RABV strains. GRP-60367 shows specific and potent anti-RABV activity of the scaffold, returning in dose-response assays EC 50 s ranging from 2 to 52 nM on different host cell lines. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.829 ml | 14.146 ml | 28.291 ml |
5 mM | 0.566 ml | 2.829 ml | 5.658 ml |
10 mM | 0.283 ml | 1.415 ml | 2.829 ml |
5 mM | 0.057 ml | 0.283 ml | 0.566 ml |
biological activity | GRP-60367 is the first small molecule rabies Virus (RABV) entry inhibitor, it has a nanomolar effect on some RABV strains. |
Target | RABV |