Ebopiprant-OBE022-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEEbopiprantCat.No.:HY-112284CASNo.:2005486-31-5Synonyms:OBE022分?式:C??H??FN?O?S?分?量:599.74作?靶點(diǎn):ProstaglandinReceptor作?通路:GPCR/GProtein儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:250mg/mL(416.85mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.6674mL8.3369mL16.6739mL5mM0.3335mL1.6674mL3.3348mL10mM0.1667mL0.8337mL1.6674mL請(qǐng)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(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)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(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.08mg/mL(3.47mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.08mg/mL(3.47mM);Suspendedsolution;Needultrasonic3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(3.47mM);ClearsolutionBIOLOGICALACTIVITY?物活性Ebopiprant(OBE022)?個(gè)?服的、前列腺素F2α(PGF2α)受體的選擇性拮抗劑，其對(duì)?和??FP受體的Ki值分別為1nM和26nM。IC50&TargetHumanFPReceptorRatFPReceptor1nM(Ki)26nM(Ki)體外研究Ebopiprant(OBE022)andOBE002areassayedforFPbindingaffinitybycompetitivebindinganalysiswith3H-PGF2αusingHEK293cellsstablytransfectedwiththeFPreceptor.Bindingaffinities(Ki)ofOBE022forthehumanandratFPreceptorare1nMand26nMrespectively.ForOBE002,Kisare6nMforthehumanand313nMfortheratFPreceptor.ThebindingofbothOBE022andOBE002isreversibleandcompetitivesinceincreasingconcentrationsofeithercompoundcausessuccessivedecreasesintheslopeofthebindingcurves,consistentwithanincreaseinequilibriumdissociationconstant(KD)withoutareductioninreceptordensity[1].體內(nèi)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?邊的抑制劑?師www.MedChemEthesameexperimentaldesignassingletreatment[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.REFERENCES[1].OliverPohl,etal.OBE022,anoralandselectiveprostaglandinF2αreceptorantagonistasaneffectiveandsafemodalityforthetreatmentofpretermlabor.JPharmacolExpTher.2018Aug;366(2):349-364.McePdf