BAY-1316957-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEBAY-1316957Cat.No.:HY-111539CASNo.:1613264-40-6分⼦式:C₂₇H₂₇N₃O₃分⼦量:441.52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:100mg/mL(226.49mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.2649mL11.3245mL22.6490mL5mM0.4530mL2.2649mL4.5298mL10mM0.2265mL1.1325mL2.2649mL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%salineSolubility:≥2.08mg/mL(4.71mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥5mg/mL(11.32mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.71mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性BAY-1316957⼀种有效的，选择性的，具有⼝服活性的前列腺素E2受体亚型4(EP4-R)的拮抗剂，对⼈EP4-R的IC50为15.3nM。BAY-1316957具有出⾊的药物代谢和药代动⼒学特性，并可⽤于⼦宫内膜异位的研究。IC50&TargetIC50:15.3nM(EP4)[1]体外研究BAY-1316957(Compound32)showshighsolubilityandpermeabilityusingtheCaco-2cellularassay[1].体内研究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].BäurleS,etal.IdentificationofaBenzimidazolecarboxylicAcidDerivative(BAY1316957)asaPotentandSelectiveHumanProstaglandinE2ReceptorSubtype4(hEP4-R)AntagonistfortheTreatmentofEndometriosis.JMedChem.2019Mar14;62(5):2541-2563.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplication