ZT-1a-DataSheet-生命科学试剂-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemEZT-1aCat.No.:HY-136532CASNo.:212135-62-1分⼦式:C₂₂H₁₅Cl₃N₂O₂分⼦量:445.73作⽤靶点:Others作⽤通路:Others储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:125mg/mL(280.44mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.2435mL11.2176mL22.4351mL5mM0.4487mL2.2435mL4.4870mL10mM0.2244mL1.1218mL2.2435mL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，并请注意储备液的保存⽅式和期限。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，配制前请先配制澄的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的⼯作液，建议您现⽤现配，当天使⽤；澄的储备液可以根据储存条件，适当保存；以下溶剂前的百分⽐指该溶剂在您配制终溶液中的体积占⽐)：1.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(4.67mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.67mM);ClearsolutionBIOLOGICALACTIVITY1/2MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemE⽣物活性ZT-1a⼀种有效的⾮ATP竞争性的选择性SPAK抑制剂。ZT-1a抑制SPAK活性，在ATP浓度为0.01、0.1和1mM时，IC50分别为44.3、35.0、46.7μM[1]。IC50&TargetSPAK[1]体外研究ZT-1ainhibitsNa-K-2Clcotransporter(NKCC1)andstimulatesK-Clcotransporters(KCCs)bydecreasingtheirSPS1-relatedproline/alanine-richkinase(SPAK)-dependentphosphorylation[1].ZT-1ainhibitsphosphorylationofNKCC1p-Thr203/207/212by72±5.2%at1ꢀµMZT-1aandphosphorylationofKCCsites1/2by65-77%at3ꢀµMinHEK-293cells[1].SPAKphosphorylationatSer373isinhibitedby70±3.8%inhibitionat3-10ꢀµMZT-1a[1].ZT-1a(10ꢀµM)inhibitsNKCC1butstimulatesKCC3activity[1].体内研究ZT-1a(10-100ꢀmg/kg)inhibitsSPAK-dependentcation-Cl−cotransporters(CCC)phosphorylationinvivo[1].AnimalModel:Naivemice[1]Dosage:10,30,50,and100ꢀmg/kgAdministration:Intraperitoneal(i.p.)administrationResult:InhibitedSPAK-dependentcation-Cl-cotransporters(CCC)phosphorylationinvivo.REFERENCES[1].JinweiZhang,etal.ModulationofBraincation-Cl-CotransportviatheSPAKKinaseInhibitorZT-1a.NatCommun.2020Jan7;11(1):78.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Te