Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemE5-BDBDCat.No.:HY-101911CASNo.:768404-03-1分?式:C??H??BrN?O?分?量:355.19作?靶點:P2XReceptor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:62.5mg/mL(175.96mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.8154mL14.0770mL28.1539mL5mM0.5631mL2.8154mL5.6308mL10mM0.2815mL1.4077mL2.8154mL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；?旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內使?，-20°C儲存時，請在1個?內使?。體內實驗請根據(jù)您的實驗動物和給藥?式選擇適當?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當保存；體內實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(5.86mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(5.86mM);ClearsolutionBIOLOGICALACTIVITY?物活性5-BDBD?種有效的選擇性P2X4受體拮抗劑，抑制rP2X4R介導的電流，其IC50為0.75μM。5-BDBD可完全阻斷硝酸?油(NTG)誘導的礎性和急性痛覺過敏[1][2]。IC50&TargetI50:0.75μM(P2X4receptor)體外研究5-BDBDinhibits10μMATP-inducedcurrentsofrP2X4R-expressingHEK293cellsinaconcentration-dependentmanner,withanIC50of0.75μM[1].5-BDBDdisplacesrightwardtheATPconcentration-responsecurve,withanEC50of4.7to15.9μM[1].5-BDBDcouldbespecificallyusedtodiscriminatebetweenP2X1R,P2X2aR,P2X2bR,P2X3R,P2X4R,andP2X7R[1].體內研究5-BDBD(28mg/kg;i.p.;dailyfor9days)cancompletelyblockethebasalhyperalgesiainducedbyrecurrentNTGinjection[2].AnimalModel:MaleC57BL/6mice[2]Dosage:28mg/kgAdministration:I.p.;dailyfor9daysResult:PreventedNTG-inducedmechanicalhypersensitivity.REFERENCES[1].CoddouC,etal.Characterizationoftheantagonistactionsof5-BDBDattheratP2X4receptor.NeurosciLett.2019;690:219-224.[2].LongT,etal.MicrogliaP2X4receptorcontributestocentralsensitizationfollowingrecurrentnitroglycerinstimulation.JNeuroinflammation.2018;15(1):245.Published2018Aug30.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuse