2170696-76-9
2170696-76-9 structure
- Name: PfKRS1 inhibitor 5
- Chemical Name: LysRs-IN-2
- CAS Number: 2170696-76-9
- Molecular Formula: C17H16F3NO4
- Molecular Weight: 355.31
- Catalog: Research Areas Infection
- Create Date: 2019-06-06 20:17:13
- Modify Date: 2024-03-04 21:02:46
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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].
| Name | LysRs-IN-2 |
|---|
| 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]. |
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| Related Catalog | |
| 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. |
| References |
| Molecular Formula | C17H16F3NO4 |
|---|---|
| Molecular Weight | 355.31 |