Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEBAY-1316957Cat.No.:HY-111539CASNo.:1613264-40-6分?式:C??H??N?O?分?量:441.52作?靶點:ProstaglandinReceptor作?通路:GPCR/GProtein儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:100mg/mL(226.49mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.2649mL11.3245mL22.6490mL5mM0.4530mL2.2649mL4.5298mL10mM0.2265mL1.1325mL2.2649mL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(dāng)?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(dāng)保存；體內(nèi)實驗的?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.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(4.71mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥5mg/mL(11.32mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.71mM);ClearsolutionBIOLOGICALACTIVITY?物活性BAY-1316957?種有效的，選擇性的，具有?服活性的前列腺素E2受體亞型4(EP4-R)的拮抗劑，對?EP4-R的IC50為15.3nM。BAY-1316957具有出?的藥物代謝和藥代動?學(xué)特性，并可?于?宮內(nèi)膜異位的研究。IC50&TargetIC50:15.3nM(EP4)[1]體外研究BAY-1316957(Compound32)showshighsolubilityandpermeabilityusingtheCaco-2cellularassay[1].體內(nèi)研究BAY-1316957(Compound32;0.2-5mg/kg;oraladministration;once)treatmentsignificantlyreducesmechanicalallodyniaindmPGE2painmodel[1].ThepharmacokineticparametersofBAY-1316957(Compound32)showsalowclearance,longhalf-life,andhighbioavailability(F%=90%)inWistarrats.InvestigationofthemetabolicpathwaysofBAY-1316957(Compound32)inhuman,rat,mouse,dog,andmonkeyhepatocytesrevealedthattheformationoftheacylglucuronidewasalsothecommonandpredominantrouteofbiotransformation,mainlycatalyzedbyUGT1A1andtoalesserextentbyUGT1A3[1].AnimalModel:MaleadultSpragueDawleyrats(220-265g)injectedwith16,16-dimethylprostaglandinE2(dmPGE2)[1]Dosage:0.2mg/kg,1mg/kg,5mg/kgAdministration:Oraladministration;onceResult:SignificantlyreducedpawwithdrawalthresholdsindmPGE2painmodel.REFERENCES[1].B?urleS,etal.IdentificationofaBenzimidazolecarboxylicAcidDerivative(BAY1316957)asaPotentandSelectiveHumanProstaglandinE2ReceptorSubtype4(hEP4-R)AntagonistfortheTreatmentofEndometriosis.JMedChem.2019Mar14;62(5):2541-2563.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplication