LysRs-IN-2 is a lysyl-tRNA synthetase (KRS) inhibitor with IC 50 s of 0.015 μM and 0.13 μM for Plasmodium falciparum lysyl-tRNA synthetase (PfKRS) and Cryptosporidium parvum lysyl-tRNA synthetase (CpKRS), respectively.
性状
Solid
IC50 & Target[1][2]
IC50: 0.015 μM (PfKRS), 0.13 μM (CpKRS)
体外研究(In Vitro)
LysRs-IN-2 is active against whole-cell bloodstream P. falciparum 3D7 (EC50=0.27 μM), Hs KRS (IC50=1.8 μM), HepG2 cells (EC50=49 μM), and Cryptosporidium parvum (EC50=2.5 μM). has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
LysRs-IN-2 (1.5 mg/kg; orally once a day for 4 days) reduces parasitemia by 90% in the murine P. falciparum SCID model. LysRs-IN-2 (20 mg/kg; orally once a day for 7 days) reduces parasite shedding in NOD SCID gamma mice and INF-γ-knockout mice (Cryptosporidium mouse models). has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
参考文献
[1]. Baraga?a B, et al. Lysyl-tRNA synthetase as a drug target in malaria and cryptosporidiosis. Proc Natl Acad Sci U S A. 2019 Apr 2;116(14):7015-7020.