Rac-Modipafant-UK-74505-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemE(Rac)-ModipafantCat.No.:HY-108908CASNo.:122956-68-7Synonyms:UK-74505分?式:C??H??ClN?O?分?量:605.09作?靶點:Others作?通路:Others儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:50mg/mL(82.63mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.6526mL8.2632mL16.5265mL5mM0.3305mL1.6526mL3.3053mL10mM0.1653mL0.8263mL1.6526mL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，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。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。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(jié)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(nèi)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%saline1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.5mg/mL(4.13mM);ClearsolutionBIOLOGICALACTIVITY?物活性(Rac)-Modipafant(UK-74505)?種?服的、選擇性的、長效的不可逆??板活化因?受體(PAFR)受體拮抗劑。(Rac)-Modipafant預(yù)防嚴重登?熱感染。體內(nèi)研究(Rac)-Modipafant(UK-74505)(10mg/kg;p.o.;twiceadayuntilday10)preventsSevereDengueInfection[3].(Rac)-Modipafantexhibitshighlyselective,time-dependentinhibitionofPAF-inducedaggregationofrabbitwashedplatelets(IC50=26.3and1.12nMafter0.25and60minpreincubation,respectively)[4].(Rac)-Modipafant(5-20mg/kg;p.o.)dose-dependentlyinhibitstheZymosan-inducedarticularhyperalgesia[5].AnimalModel:8-to10-week-oldBALB/cmice(DEN-2straininfected)[3]Dosage:10mg/kgAdministration:P.o.;twiceaday(startedondays0,3,5,or7)untilday10Result:Decreasedbyapproximately50%thelethalityassociatedwithDEN-2infection.AnimalModel:MaleBALB/C(8-to10-week-old)wild-typemice[5]Dosage:5,10and20mg/kgAdministration:P.o.Result:Dose-dependentlyinhibitedtheZymosan-inducedarticularhyperalgesia.REFERENCES[1].O'ConnorBJ,etal.InhibitoryeffectofUK,74505,apotentandspecificoralplateletactivatingfactor(PAF)receptorantagonist,onairwayandsystemicresponsestoinhaledPAFinhumans.AmJRespirCritCareMed.1994;150(1):35-40.[2].AlabasterVA,etal.UK-74,505,anovelandselectivePAFantagonist,exhibitspotentandlonglastingactivityinvivo.AgentsActionsSuppl.1991;34:221-227.[3].ParryMJ,AlabasterVA,etal.PharmacologicalprofileofUK-74,505,anovelandselectivePAFantagonistwithpotentandprolongedoralactivity.JLipidMediatCellSignal.1994;10(3):251-268.[4].GuerreroAT,etal.TheroleofPAF/PAFRsignalinginzymosan-inducedarticularinflammatoryhyperalgesia[publishedcorrectionappearsinNaunynSchmiedebergsArchPharmacol.2013Apr;386(4):351.Zaperlon,AnaC[correctedtoZarpelon,AnaC]].NaunynSc[5].SouzaDG,etal.Essentialroleofplatelet-activatingfactorreceptorinthepathogenesisofDenguevirusinfection.ProcNatlAcadSciUSA.2009;106(33):14138-14143.McePdfHeight2/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemECaution:Producthasnotbeenfullyvalidated