Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemEKCC2blocker1Cat.No.:HY-18172CASNo.:1228439-36-8分?式:C??H??NO?S分?量:415.5作?靶點:PotassiumChannel作?通路:MembraneTransporter/IonChannel儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:250mg/mL(601.68mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.4067mL12.0337mL24.0674mL5mM0.4813mL2.4067mL4.8135mL10mM0.2407mL1.2034mL2.4067mL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>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(5.01mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(5.01mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(5.01mM);Clearsolution1/2MasterofSmallMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性KCC2blocker1?種?服有效的，選擇性的K+-Cl-共轉(zhuǎn)運蛋?KCC2阻滯劑，IC50為1μM。KCC2blocker1?種脯氨酸芐酯，具有抗癲癇作?。IC50&TargetIC50:1μM(KCC2)[1]體外研究KCC2blocker1(compound13;100μM)inhibitsNKCC1with35%.體內(nèi)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