Catalog No.: PC-49292Not For Human Use, Lab Use Only.
DDD01510706 is a small molecule inhibitor of PfKRS (Plasmodium falciparum Lysyl tRNA Synthetase) with pIC50 of 6.62, interacts with the ATP binding site of PfKRS, inhibits plasmodium falciparum asexual blood-stage (ABS) parasite strain Dd2 with EC50 of 0.3 uM.
DDD01510706 (DDD706) isa potent, selective inhibitor of apicomplexan lysyl-tRNA synthetase (KRS) with IC50 of 0.015 uM and 0.13 uM for PfKRS1 and CpKRS respectively, Pf(3D7) EC50 of 0.27 uM.
DDD706 is selective over (human) HsKRS (IC50=1.8 uM).
DDD706 is active against both PfKRS1 (IC50 = 0.015 μM) and whole-cell bloodstream P. falciparum 3D7 (EC50 = 0.27 μM) and is selective compared with both the HsKRS (IC50 = 1.8 μM) and HepG2 cells (EC50 = 49 μM).
DDD706 shows activity against parasites resistant to chloroquine Pf(K1) (EC50 = 0.51 μM) or atovaquone Pf(TM90C2B) (EC50 = 0.52 μM) is similar to the drug-sensitive strain Pf(NF54) (EC50 = 0.39 μM).
DDD706 shows comparable activity in liver schizonts (P. vivax liver schizont EC50 = 0.95 μM) to asexual blood stages.
DDD706 shows in vivo activity in mouse models of malaria and cryptosporidiosis infections.
