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LysRs-IN-2 is a lysine tRNA synthetase (KRS) inhibitor with antiparasitic activity that inhibits Plasmodium falciparum KRS (PfKRS) and Cryptosporidium minum KRS (CpKRS), and is used in the study of malaria infections.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $112 | In Stock | |
5 mg | $328 | In Stock | |
10 mg | $519 | In Stock | |
25 mg | $833 | In Stock | |
50 mg | $1,130 | In Stock | |
100 mg | $1,530 | In Stock | |
200 mg | $1,980 | In Stock |
Description | LysRs-IN-2 is a lysine tRNA synthetase (KRS) inhibitor with antiparasitic activity that inhibits Plasmodium falciparum KRS (PfKRS) and Cryptosporidium minum KRS (CpKRS), and is used in the study of malaria infections. |
Targets&IC50 | Cryptosporidium minis:2.5 μM (EC50), CpKRS:0.13 μM, HepG2 cells:49 μM (EC50), PfKRS:0.015 μM, P. falciparum strain 3D7:0.27 μM (EC50), lysyl-tRNA synthetase (HsKRS) (human):1.8 μM |
In vitro | LysRs-IN-2 is a lysyl-tRNA synthetase (KRS) inhibitor with half inhibitory concentrations (IC50) of 0.015 μM and 0.13 μM for Plasmodium falciparum lysyl-tRNA synthetase (PfKRS) and Cryptosporidium lysyl-tRNA synthetase (CpKRS) respectively.[1] LysRs-IN-2 showed significant activity against P. falciparum strain 3D7 (EC50=0.27 μM), human lysyl-tRNA synthetase (HsKRS) (IC50=1.8 μM), HepG2 cells (EC50=49 μM), and Cryptosporidium minis (EC50=2.5 μM) in a whole-cell assay. [1] |
In vivo | In the P. falciparum SCID mouse model, LysRs-IN-2 (1.5 mg/kg; orally once daily for 4 days) reduced parasitemia levels by 90%. In NOD SCID gamma mice and INF-γ knockout mice (Cryptosporidium minis model), LysRs-IN-2 (20 mg/kg; orally once daily for 7 days) significantly reduced parasite excretion. [1] |
Molecular Weight | 355.31 |
Formula | C17H16F3NO4 |
Cas No. | 2170696-76-9 |
Smiles | O=C1C=C(OC2=CC=C(F)C=C12)C(=O)NCC3(O)CCC(F)(F)CC3 |
Relative Density. | 1.44 g/cm3 (Predicted) |
Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 50.00 mg/mL (140.72 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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