GSK726701A-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEGSK726701ACat.No.:HY-112152CASNo.:945721-87-9分?式:C??H??FNO?分?量:423.43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:25mg/mL(59.04mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.3617mL11.8083mL23.6167mL5mM0.4723mL2.3617mL4.7233mL10mM0.2362mL1.1808mL2.3617mL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>>90%cornoilSolubility:≥2.5mg/mL(5.90mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性GSK726701A前列腺素E2受體4(EP4)的部分激動劑，pEC50為7.4。IC50&TargetpEC50:7.4[1]體外研究GSK726701Ahashighselectivity(>100-fold)againstasetofotherprostaglandinreceptors(EP1-3,DP1,FP,IP,TP)andnosignificantactivityagainstawiderpaneloftargets.ItdemonstratesEP4agonistactivitywithsimilarpotencyandintrinsicactivity(pEC50=8.2)inahumanwholeblood(HWB)assayontheinhibitionofLPS-mediatedTNFαinduction[1].體內(nèi)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