LysRs-IN-2-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemELysRs-IN-2Cat.No.:HY-126130CASNo.:2170696-76-9分⼦式:C₁₇H₁₆F₃NO₄分⼦量:355.31作⽤靶点:Aminoacyl-tRNASynthetase作⽤通路:MetabolicEnzyme/Protease储存⽅式:4°C,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(storedunder

nitrogen)溶解性数据体外实验DMSO:≥60mg/mL(168.87mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM2.8144mL14.0722mL28.1444mL5mM0.5629mL2.8144mL5.6289mL10mM0.2814mL1.4072mL2.8144mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month(storedundernitrogen)。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(5.85mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥1.5mg/mL(4.22mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥1.5mg/mL(4.22mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性LysRs-IN-2⼀种赖氨酸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0.015μM、0.13μM[1]。IC50&TargetIC50:0.015μM(PfKRS),0.13μM(CpKRS)[1]体外研究LysRs-IN-2isactiveagainstwhole-cellbloodstreamP.falciparum3D7(EC50=0.27μM),HsKRS(IC50=1.8μM),HepG2cells(EC50=49μM),andCryptosporidiumparvum(EC50=2.5µM)[1].体内研究LysRs-IN-2(1.5mg/kg;orallyonceadayfor4days)reducesparasitemiaby90%inthemurineP.falciparumSCIDmodel.LysRs-IN-2(20mg/kg;orallyonceadayfor7days)reducesparasitesheddinginNODSCIDgammamiceandINF-γ-knockoutmice(Cryptosporidiummousemodels)[1].AnimalModel:MurineP.falciparumNODscidIL2Rγnull(SCID)model[1]Dosage:1.5mg/kgAdministration:Orallyonceadayfor4daysResult:Reducedparasitemiaby90%inthemalariaSCIDmousemodel.AnimalModel:NODSCIDgammaandINF-γ–knockoutmousemodels(Cryptosporidiummousemodels)[1]Dosage:20mg/kgAdministration:Orallyonceadayfor7daysResult:Reducedparasitesheddingbelowdetectionlevel,andthisreductionwassustainedfor3wkaftertreatmenthadstoppedinINF-γ-knockoutmice.Dosedorallyataconcentrationof20mg/kgonceadayfor7daysshowed96%reductionofparasitesheddingcomparabletoparomomycininNODSCIDgammamice.REFERENCES[1].BaragañaB,etal.Lysyl-tRNAsynthetaseasadrugtargetinmalariaandcryptosporidiosis.ProcNatlAcadSciUSA.2019Apr2;116(14):7015-7020.McePdfHeight2/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemECaution:Producthasnotbeenfullyvalidatedformedicala