1. Metabolic Enzyme/Protease
  2. Aminoacyl-tRNA Synthetase

LysRs-IN-2 

目录号: HY-126130
产品使用指南

LysRs-IN-2 是一种赖氨酸 tRNA 合成酶 ((KRS)) 抑制剂,其对恶性疟原虫 KRS (PfKRS) 和小隐孢子虫 KRS (CpKRS) 的 IC50 值分别为 0.015 μM、0.13 μM。

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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.
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

Storage

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

Shipping

Room temperature in continental US; may vary elsewhere

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产品名称:
LysRs-IN-2
目录号:
HY-126130
需求量:

LysRs-IN-2

Cat. No.: HY-126130