1. Metabolic Enzyme/Protease
  2. Aminoacyl-tRNA Synthetase
  3. LysRs-IN-2

LysRs-IN-2 

Cat. No.: HY-126130
Handling Instructions

LysRs-IN-2 is a lysyl-tRNA synthetase (KRS) inhibitor with IC50s of 0.015 μM and 0.13 μM for Plasmodium falciparum lysyl-tRNA synthetase (PfKRS) and Cryptosporidium parvum lysyl-tRNA synthetase (CpKRS), respectively.

For research use only. We do not sell to patients.

LysRs-IN-2 Chemical Structure

LysRs-IN-2 Chemical Structure

CAS No. : 2170696-76-9

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Description

LysRs-IN-2 is a lysyl-tRNA synthetase (KRS) inhibitor with IC50s of 0.015 μM and 0.13 μM for Plasmodium falciparum lysyl-tRNA synthetase (PfKRS) and Cryptosporidium parvum lysyl-tRNA synthetase (CpKRS), respectively[1].

IC50 & Target

IC50: 0.015 μM (PfKRS), 0.13 μM (CpKRS)[1]

In Vitro

LysRs-IN-2 is active against whole-cell bloodstream P. falciparum 3D7 (EC50 = 0.27 μM), HsKRS (IC50 = 1.8 μM), HepG2 cells (EC50 = 49 μM), and Cryptosporidium parvum (EC50 = 2.5 µM)[1].

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)[1].

Animal Model: Murine P. falciparum NODscidIL2Rγnull (SCID) model[1]
Dosage: 1.5 mg/kg
Administration: Orally once a day for 4 days
Result: Reduced parasitemia by 90% in the malaria SCID mouse model.
Animal Model: NOD SCID gamma and INF-γ–knockout mouse models (Cryptosporidium mouse models)[1]
Dosage: 20 mg/kg
Administration: Orally once a day for 7 days
Result: Reduced parasite shedding below detection level, and this reduction was sustained for 3 wk after treatment had stopped in INF-γ-knockout mice. Dosed orally at a concentration of 20 mg/kg once a day for 7 days showed 96% reduction of parasite shedding comparable to paromomycin in NOD SCID gamma mice.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
Molecular Weight

355.31

Formula

C₁₇H₁₆F₃NO₄

CAS No.

2170696-76-9

SMILES

FC1=CC=C(OC(C(NCC2(O)CCC(F)(F)CC2)=O)=CC3=O)C3=C1

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Room temperature in continental US; may vary elsewhere

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LysRs-IN-2
Cat. No.:
HY-126130
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LysRs-IN-2

Cat. No.: HY-126130