P2X3-antagonist-34-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemEP2X3antagonist34Cat.No.:HY-135976CASNo.:2417288-67-4分⼦式:C₂₄H₂₆F₂N₄O₃分⼦量:456.49作⽤靶点:P2XReceptor作⽤通路:MembraneTransporter/IonChannel储存⽅式:-20°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)溶解性数据体外实验DMSO:100mg/mL(219.06mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.1906mL10.9531mL21.9063mL5mM0.4381mL2.1906mL4.3813mL10mM0.2191mL1.0953mL2.1906mL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:≥2.5mg/mL(5.48mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(5.48mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.48mM);Clearsolution1/2MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性P2X3antagonist34⼀种有效的，选择性的，⼝服活性的P2X3同型三聚体受体拮抗剂，对⼈P2X3，⼤⿏P2X3和豚⿏P2X3受体的IC50分别为25nM，92nM和126nM。P2X3antagonist34对⼈，⼤⿏和豚⿏P2X2/3异三聚体受体的活性较低。P2X3antagonist34具有很强的镇咳作⽤。IC50&TargetIC50:25ꢀnM(HumanP2X3receptor),92ꢀnM(RatP2X3receptor)and126ꢀnM(GuineapigP2X3receptor),1820nM(RatP2X2/3heterotrimericreceptor)and3450nM(GuineapigP2X2/3heterotrimericreceptor)[1]体外研究P2X3antagonist34(BLU-5937;500ꢀnM)isabletoblockαβ-meATP-inducedsensitizationandfiringactivityofisolatedprimarynociceptorsinratdorsalrootganglions(DRGs),throughP2X3homotrimericreceptorantagonism.Thesensitizingeffectofαβ-meATPandtheinhibitionofP2X3antagonist34arereversibleafterwashout[1].体内研究P2X3antagonist34(BLU-5937;0.3-0ꢀmg/kg,oraladministration;maleDunkinHartleyguineapigs)treatmentsignificantlyreducesthehistamine-inducedenhancementinthenumberofcitricacid-inducedcoughsinadose-dependentfashioninaguineapigcoughmodel[1].P2X3antagonist34(BLU-5937;3and30ꢀmg/kg,oral)isalsoshowntoreducesignificantlyanddose-dependentlytheATP-inducedenhancementofcitricacid-inducedcoughsintheguineapig[1].AnimalModel:MaleDunkinHartleyguineapigs[1]Dosage:0.3mg/kg,3mg/kg,30ꢀmg/kgAdministration:OraladministrationResult:Significantlyreducedthehistamine-inducedenhancementinthenumberofcitricacid-inducedcoughsinadose-dependentfashion.REFERENCES[1].GarceauD,etal.BLU-5937:AselectiveP2X3antagonistwithpotentanti-tussiveeffectandnotastealteration.PulmPharmacolTher.2019Jun;56:56-62.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalap