ZT-1a-DataSheet-生命科學試劑-生命科學試劑-MedChemExpressVIP

Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemEZT-1aCat.No.:HY-136532CASNo.:212135-62-1分?式:C??H??Cl?N?O?分?量:445.73作?靶點:Others作?通路:Others儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:125mg/mL(280.44mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.2435mL11.2176mL22.4351mL5mM0.4487mL2.2435mL4.4870mL10mM0.2244mL1.1218mL2.2435mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存?式和期限。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當?shù)娜芙?案，配制前請先配制澄的儲備液，再依次添加助溶劑(為保證實驗結(jié)果的可靠性，體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；澄的儲備液可以根據(jù)儲存條件，適當保存；以下溶劑前的百分?指該溶劑在您配制終溶液中的體積占?)：1.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(4.67mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.67mM);ClearsolutionBIOLOGICALACTIVITY1/2MasterofSmallMolecules—您?邊的抑制劑?師www.MedChemE?物活性ZT-1a?種有效的?ATP競爭性的選擇性SPAK抑制劑。ZT-1a抑制SPAK活性，在ATP濃度為0.01、0.1和1mM時，IC50分別為44.3、35.0、46.7μM[1]。IC50&TargetSPAK[1]體外研究ZT-1ainhibitsNa-K-2Clcotransporter(NKCC1)andstimulatesK-Clcotransporters(KCCs)bydecreasingtheirSPS1-relatedproline/alanine-richkinase(SPAK)-dependentphosphorylation[1].ZT-1ainhibitsphosphorylationofNKCC1p-Thr203/207/212by72±5.2%at1?μMZT-1aandphosphorylationofKCCsites1/2by65-77%at3?μMinHEK-293cells[1].SPAKphosphorylationatSer373isinhibitedby70±3.8%inhibitionat3-10?μMZT-1a[1].ZT-1a(10?μM)inhibitsNKCC1butstimulatesKCC3activity[1].體內(nèi)研究ZT-1a(10-100?mg/kg)inhibitsSPAK-dependentcation-Cl?cotransporters(CCC)phosphorylationinvivo[1].AnimalModel:Naivemice[1]Dosage:10,30,50,and100?mg/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