Ebopiprant-OBE022-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEEbopiprantCat.No.:HY-112284CASNo.:2005486-31-5Synonyms:OBE022分⼦式:C₃₀H₃₄FN₃O₅S₂分⼦量:599.74作⽤靶点:ProstaglandinReceptor作⽤通路:GPCR/GProtein储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:250mg/mL(416.85mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.6674mL8.3369mL16.6739mL5mM0.3335mL1.6674mL3.3348mL10mM0.1667mL0.8337mL1.6674mL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%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.08mg/mL(3.47mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.08mg/mL(3.47mM);Suspendedsolution;Needultrasonic3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(3.47mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Ebopiprant(OBE022)⼀个⼝服的、前列腺素F2α(PGF2α)受体的选择性拮抗剂，其对⼈和⼤⿏FP受体的Ki值分别为1nM和26nM。IC50&TargetHumanFPReceptorRatFPReceptor1nM(Ki)26nM(Ki)体外研究Ebopiprant(OBE022)andOBE002areassayedforFPbindingaffinitybycompetitivebindinganalysiswith3H-PGF2αusingHEK293cellsstablytransfectedwiththeFPreceptor.Bindingaffinities(Ki)ofOBE022forthehumanandratFPreceptorare1nMand26nMrespectively.ForOBE002,Kisare6nMforthehumanand313nMfortheratFPreceptor.ThebindingofbothOBE022andOBE002isreversibleandcompetitivesinceincreasingconcentrationsofeithercompoundcausessuccessivedecreasesintheslopeofthebindingcurves,consistentwithanincreaseinequilibriumdissociationconstant(KD)withoutareductioninreceptordensity[1].体内研究Time-courseofthecumulativepercentageofdeliversmiceafterRU486-inducedpretermparturitionatGD17,inOBE022,nifedipineorvehicletreatmentgroups.OraltreatmentwithOBE022delaysthepretermbirthcausedbyRU486administrationasreflectedbyashifttotherightofthepercentageofdeliverycurve.Theeffectoforaltreatmentwithnifedipineiscomparable.BothOBE022andnifedipineshowatrendtoincreasethetimeoffirstpupdelivery.Asanimportantconsequenceoftheprolongationofgestation,damsdeliverviablepups.CombinationofOBE022andnifedipinecauseasynergisticeffectonthedelayofRU486-inducedpretermbirthasreflectedbyamorepronouncedshifttotherightofthepercentageofdeliverycurve,incomparisontoOBE022ornifedipinealone.Also,alargerincreaseofthetimeoffirstpupdeliveryisobserved[1].PROTOCOLAnimalMice[1]Administration[1]PrimigravidCD1mice,onday17ofpregnancy(about85%gestation)atthebeginningoftheexperiments,areused.Approximately3hoursbeforeinductionofpretermlabor(Day1(D1)at10h00),thepregnantmiceatgestationalday17,areplacedinindividualcageswithfoodandwateradlibitum.PregnantmicereceiveonD1(atdaytime:13h00)asinglesubcutaneous(s.c.)injectionofRU486atadoseof2.5mg/kginafinalvolumeof10mL/kgofsesameoil.OBE022(10,30and100mg/kg)ornifedipine(5mg/kg)areadministeredorally(p.o.)atavolumeof5mL/kgonceonD1(18h00),twiceonD2(8h00and18h00)andonceonD3(8h00)foratotalof4administrations.Forcombinationtreatment,micereceiveOBE022plusnifedipineusing2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEthesameexperimentaldesignassingletreatment[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.REFERENCES[1].OliverPohl,etal.OBE022,anoralandselectiveprostaglandinF2αreceptorantagonistasaneffectiveandsafemodalityforthetreatmentofpretermlabor.JPharmacolExpTher.2018Aug;366(2):349-364.McePdf