Rac-Modipafant-UK-74505-DataSheet-生命科学试剂-MedChemExpressVIP

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemE(Rac)-ModipafantCat.No.:HY-108908CASNo.:122956-68-7Synonyms:UK-74505分⼦式:C₃₄H₂₉ClN₆O₃分⼦量:605.09作⽤靶点:Others作⽤通路:Others储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:50mg/mL(82.63mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.6526mL8.2632mL16.5265mL5mM0.3305mL1.6526mL3.3053mL10mM0.1653mL0.8263mL1.6526mL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；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。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。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(4.13mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性(Rac)-Modipafant(UK-74505)⼀种⼝服的、选择性的、长效的不可逆⾎⼩板活化因⼦受体(PAFR)受体拮抗剂。(Rac)-Modipafant预防严重登⾰热感染。体内研究(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—您⾝边的抑制剂⼤师www.MedChemECaution:Producthasnotbeenfullyvalidated