产品
编 号：F275461
分子式：C17H16F3NO4
分子量：355.31
分子式：C17H16F3NO4
分子量：355.31
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
结构图
CAS No: 2170696-76-9
产品详情
生物活性：
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.
体内研究：
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).Animal Model:Murine P. falciparum NODscidIL2Rγnull (SCID) model
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)
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.
体外研究：
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).
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.
体内研究：
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).Animal Model:Murine P. falciparum NODscidIL2Rγnull (SCID) model
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)
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.
体外研究：
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).
产品资料
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