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GSK1292263isanovelGPR119receptoragonistusedforthetreatmentoftype2diabetes.ThepredictedEC50ofGSK1292263againstGPR119invitroisatthenanomolarrange.(1)TheGPR119receptorisaGPCRwhichisselectivelyexpressedonpancreaticbetacellsandintestinalenteroendocrinecells.AgoniststoGPR119stimulateglucose-dependentinsulinsecretioninvitroandloweranelevatedbloodglucoselevelinvivo.(2)
Invivo,GSK1292263treatmentsignificantlyincreasesinthepeakinsulinresponseandinsulinAUC(0-15min)by30-60%comparedwithvehiclecontrolintheintravenousglucosetolerancetest.Thisinsulinupregulationcorrelatedwithasignificantincreaseintheglucosedisposalrate.(3)
Technicalinformation:
| ChemicalFormula: | C23H28N4O4S | |
| CAS#: | 1032823-75-8 | |
| MolecularWeight: | 456.56 | |
| Purity: | >98% | |
| Appearance: | white | |
| ChemicalName: | 3-isopropyl-5-(4-(((6-(4-(methylsulfonyl)phenyl)pyridin-3-yl)oxy)methyl)piperidin-1-yl)-1,2,4-oxadiazole | |
| Solubility: | Upto100mMinDMSO | |
| Synonyms: | GSK1292263,GSK1292263,GSK-1292263 |
ShippingCondition:Theproductisshippedinaglassvialatambienttemperature.
Storagecondition:Forlongershelflife,storesolidpowderat4oCdesiccated,orstoreDMSOsolutionat-20oC.
Reference:
| 1. | ZhuXetal.,ThefirstpharmacophoremodelforpotentGprotein-coupledreceptor119agonist.EurJMedChem.2011,46(7):2901-7PubmedID:21524831 |
| 2. | OvertonHA,etal.,GPR119,anovelGprotein-coupledreceptortargetforthetreatmentoftype2diabetesandobesity.BrJPharmacol.2008,153Suppl1:S76-81.PubmedID:18037923 |
| 3. | Brown,K.K.etal.Diabetes[70thAnnuMeetSciSessAmDiabetesAssoc(ADA)(June25-29,Orlando)2010]2010,59(Suppl.1):Abst407 |