GSK726701A-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEGSK726701ACat.No.:HY-112152CASNo.:945721-87-9分⼦式:C₂₄H₂₂FNO₅分⼦量:423.43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:25mg/mL(59.04mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.3617mL11.8083mL23.6167mL5mM0.4723mL2.3617mL4.7233mL10mM0.2362mL1.1808mL2.3617mL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>>90%cornoilSolubility:≥2.5mg/mL(5.90mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性GSK726701A前列腺素E2受体4(EP4)的部分激动剂，pEC50为7.4。IC50&TargetpEC50:7.4[1]体外研究GSK726701Ahashighselectivity(>100-fold)againstasetofotherprostaglandinreceptors(EP1-3,DP1,FP,IP,TP)andnosignificantactivityagainstawiderpaneloftargets.ItdemonstratesEP4agonistactivitywithsimilarpotencyandintrinsicactivity(pEC50=8.2)inahumanwholeblood(HWB)assayontheinhibitionofLPS-mediatedTNFαinduction[1].体内研究GSK726701Ahasgoodpharmacokineticfileinrat,dogandmonkey.GSK726701AhasrobustactivityinarangeofanimalmodelsofinflammatoryandneuropathicpainGSK726701Ademonstratesatime-dependant,fullreversalofCCI-inducedmechanicalallodyniaat3mg/kg,equivalenttotheclinicalgoldstandardgabapentin(30mg/kg).GSK726701AhasanED50of0.2mg/kgintheFCAacuteratmodelofinflammatorypain[1].PROTOCOLAnimalRats[1]Administration[1]TheeffectofGSK726701A(0.03-1mg/kgp.o.b.i.d.x5days)isinvestigatedontheFCAacuteratmodelofinflammatorypain[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.REFERENCES[1].HealyMP,etal.Discoveryof{4-[4,9-bis(ethyloxy)-1-oxo-1,3-dihydro-2H-benzo[f]isoindol-2-yl]-2-fluorophenyl}aceticacid(GSK726701A),anovelEP4receptorpartialagonistforthetreatmentofpain.BioorgMedChemLett.2018Jun1;28(10):1892-1896.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresear