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Chemical Structure : PfKRS1 inhibitor 5
Catalog No.: PC-36147Not For Human Use, Lab Use Only.
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).
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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.
| M.Wt | 355.313 | |
| Formula | C17H16F3NO4 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Baragaña B, et al. Proc Natl Acad Sci U S A. 2019 Apr 2;116(14):7015-7020.
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