WNK463-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEWNK463Cat.No.:HY-100626CASNo.:2012607-27-9分⼦式:C₂₁H₂₄F₃N₇O₂分⼦量:463.46作⽤靶点:Ser/ThrProtease作⽤通路:MetabolicEnzyme/Protease储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥30mg/mL(64.73mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM2.1577mL10.7884mL21.5768mL5mM0.4315mL2.1577mL4.3154mL10mM0.2158mL1.0788mL2.1577mL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。-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%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(5.39mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.39mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性WNK463⼀种⼝服的WNK激酶抑制剂，对于WNK1，WNK2，WNK3和WNK4的IC50值分别为5nM，1nM，6nM和9nM。IC50&TargetIC50:5nM(WNK1),1nM(WNK2),6nM(WNK3),and9nM(WNK4)[1]体外研究WNK463(50nM,1μΜ,10μΜ;6days;Humantissue-engineeredcorneas(hTECs))treatmentreducesphosphorylationoftheWNK1downstreamtargetsSPAK/OSR1inwoundedhTECs.WesternBlotAnalysis[2]CellLine:Humantissue-engineeredcorneas(hTECs)Concentration:50nM,1μΜ,10μΜIncubationTime:6daysResult:ReducedphosphorylationoftheWNK1downstreamtargetsSPAK/OSR1inwoundedhTECs.体内研究WNK463(1-10mg/kg;oraladministration;4hours;SpontaneouslyhypertensiveSpragueDawleyrats)treatmentproducesdose-dependentdecreasesinbloodpressureandsimultaneousincreasesinheartrateinconsciousSHRs.WNK463producessignificantanddose-dependentincreasesinurineoutputaswellasurinarysodiumandpotassiumexcretionrates.WNK463isorallybioavailableinSpragueDawleyratswithahalf-lifeof2.1hours[1].AnimalModel:SpontaneouslyhypertensiveSpragueDawleyrats(34-42weeksofage)[1]Dosage:1mg/kg,3mg/kg,or10mg/kg(Pharmacokineticstudy)Administration:Oraladministration;4hoursResult:Decreasedinbloodpressureandsimultaneousincreasesinheartrate.WNK463producedsignificantanddose-dependentincreasedinurineoutputaswellasurinarysodiumandpotassiumexcretionrates.户使⽤本产品发表的科研⽂献•NatCommun.2021Jul27;12(1):4546.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE•NatMetab.2019Jan;1(1):47-57.•Cancers.2020Mar2;12(3):575.•IntJMolSci.2022,23(20),12100.•UniversityCollegeLondon.FrancisCrickInstitute.2021Oct.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].YamadaKetal.Small-moleculeWNKinhibitionregulatescardiovascularandrenalfunction.NatChemBiol.2016Nov;12(11):896-898.[2].DesjardinsP,etal.ContributionoftheWNK1kinasetocornealwoundhealingusingthetissue-engineeredhumancorneaasaninvitromodel.JTissueEngRegenMed.2019Sep;13(9):1595-1608.McePdfHeightCaution:Producthasnotbeenfullyvali