W-84-dibromide-HDMPPA-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEW-84dibromideCat.No.:HY-100979CASNo.:21093-51-6Synonyms:HDMPPA分?式:C??H??Br?N?O?分?量:708.52作?靶點(diǎn):mAChR作?通路:GPCR/GProtein;NeuronalSignaling儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:6.25mg/mL(8.82mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.4114mL7.0570mL14.1139mL5mM0.2823mL1.4114mL2.8228mL10mM---------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(fù)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(shí)，請?jiān)?個(gè)?內(nèi)使?，-20°C儲存時(shí)，請?jiān)?個(gè)?內(nèi)使?。BIOLOGICALACTIVITY?物活性W-84(dibromide)M2-cholinoceptors的強(qiáng)變構(gòu)調(diào)節(jié)劑，它阻礙[3H]N-methylscopolamine解離。W-84(dibromide)能穩(wěn)定膽堿能拮抗劑-受體復(fù)合物。W-84(dibromide)?種?競爭性毒蕈堿?酰膽堿受體拮抗劑，具有變構(gòu)效應(yīng)。W-84(dibromide)聯(lián)合阿托品時(shí)，可有效地防?有機(jī)磷中毒[1][2][3]。1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEIC50&Targetmuscarinicacetylcholinereceptors[1]體外研究ThestabilizingeffectofW-84(dibromide)onantagonist-receptorcomplexesmayexplaintheoveradditiveprotectiveactionexertedbythecombinationofatropineandW-84(dibromide)againstorganophosphateintoxication[1].W-84(dibromide)notonlyinhibitsradioligandassociationbutalsostronglystabilizesantagonist-receptorcomplexes[2].REFERENCES[1].JepsenK,etal.Allostericstabilizationof3H-N-methylscopolaminebindinginguinea-pigmyocardiumbyanantidoteagainstorganophosphateintoxication.PharmacolToxicol.1988;63(3):163-168.[2].MohrK,etal.EquipotentallostericeffectofW84on[3H]NMS-bindingtocardiacmuscarinicreceptorsfromguinea-pig,rat,andpig.PharmacolToxicol.1992;70(3):198-200.[3].GrossmüllerM,etal.AllostericsiteinM2acetylcholinereceptors:evidenceforamajorconformationalchangeuponbindingofanorthostericagonistinsteadofanantagonist.NaunynSchmiedebergsArchPharmacol.2006;372(4):267-276.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400