Cas No.: | 2170696-76-9 |
Chemical Name: | N-((4,4-difluoro-1-hydroxycyclohexyl)methyl)-6-fluoro-4-oxo-4H-chromene-2-carboxamide |
Formula: | C17H16F3NO4 |
M.Wt: | 355.313 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | PfKRS1 inhibitor 5 is a potent, selective, oral inhibitor of P. falciparum lysyl-tRNA synthetase (PfKRS1) with IC50 of 15 nM, displays >100-fold selectivity over Human KRS (HsKRS, IC50=1.8 uM); also shows preliminary selectivity in a 44 receptor/enzyme panel with no activity at 10 uM; demonstrates activity in whole-cell bloodstream P. falciparum 3D7 with EC50 of 0.27 uM; inhibits CpKRS and C. parvum and Cryptosporidium hominis in culture, shows vivo efficacy in mouse models of malaria and cryptosporidiosis infections. |