KCC2-blocker-1-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemEKCC2blocker1Cat.No.:HY-18172CASNo.:1228439-36-8分⼦式:C₂₂H₂₅NO₅S分⼦量:415.5作⽤靶点:PotassiumChannel作⽤通路:MembraneTransporter/IonChannel储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:250mg/mL(601.68mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.4067mL12.0337mL24.0674mL5mM0.4813mL2.4067mL4.8135mL10mM0.2407mL1.2034mL2.4067mL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>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(5.01mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(5.01mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(5.01mM);Clearsolution1/2MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性KCC2blocker1⼀种⼝服有效的，选择性的K+-Cl-共转运蛋⽩KCC2阻滞剂，IC50为1μM。KCC2blocker1⼀种脯氨酸苄酯，具有抗癫痫作⽤。IC50&TargetIC50:1μM(KCC2)[1]体外研究KCC2blocker1(compound13;100μM)inhibitsNKCC1with35%.体内研究KCC2blocker1(compound13;1mg/kgivand6mg/kgpo)hasat1/2of0.3hours,aCLof26mL/min/kg,aCmaxof457ng/mLandaAUCof726ng•h/mLformaleWistarrats[1].AnimalModel:MaleWistarrats[1]Dosage:1mg/kgor6mg/kg(PharmacokineticAnalysis)Administration:IV(1mg/kg)andPO(6mg/kg)Result:Hadat1/2of0.3hours,aCLof26mL/min/kg,aCmaxof457ng/mLandaAUCof726ng•h/mL.REFERENCES[1].PégurierC,etal.BenzylprolinatederivativesasnovelselectiveKCC2blockers.BioorgMedChemLett.2010Apr15;20(8):2542-5.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820