| MolecularWeight: | 406.42 |
| Formula: | C20H17F3N2O2S |
| Purity: | ≥98% |
| CAS#: | 1371569-69-5 |
| Solubility: | DMSOupto100mM |
| ChemicalName: | 4-(3-(benzyloxy)phenyl)-2-(ethylsulfinyl)-6-(trifluoromethyl)pyrimidine |
| Storage: | Powder:4oC1year.DMSO:4oC3month;-20oC1year. |
BIOLOGicalActivity:
BETPispositiveallostericmodulatorandpartialagoNISToftheglucagon-likepeptide1(GLP-1)receptor.Itcovalentlymodifiescysteines347and438inGLP-1R.SpecificitystudieshaveshownthatithasnoactivityonGLP-2,GIP,PTHorglucagonreceptors.BETPhasbeenshowntopotentiateGLP-1R–dependentintracellularcalciummobilizationbutnotcAMPaccumulationinresponsetoGLP-1(7-36)NH2inrecombinantcelllines.Conversely,BETPcanenhancecAMPefficacyofGLP-1(9-36)NH2atGLP-1Rbutnotintracellularcalciummobilization.BETPalsopotentiatescAMPproductionofthedual-actingGLP-1R/glucagon(GCG)receptor(GCGR)agonistoxyntomodulinatGLP-1R.ItpromotesGLP-1(9-36)NH2–mediatedglucose-dependentinsulinsecretioninrodentandhumanisletpreparationsaswellasinrodentmodelsfollowingintravenousadministration.
HowtoUse:
Invitro:BETPwasusedat5-20µMinvitroandcellularassays.
Invivo:BETPwasadministeredthroughintravenousadministrationat5mg/kgtoWistarratsforIVGTT(InVivoIntravenousGlucoseToleranceTest).Formulation:10%ethanol-Solutol,20%polyethyleneglycol-400,and70%phosphate-bufferedsaline,pH7.4.
Reference:
- 1.SloopKW,etal.Novelsmallmoleculeglucagon-likepeptide-1receptoragoniststimulatesinsulinsecretioninrodentsandfromhumanislets.(2010)Diabetes.59(12):3099-107.
- 2.CheongYH,etal.Twosmallmoleculeagonistsofglucagon-likepeptide-1receptormodulatethereceptoractivationresponsedifferently.(2012)BiochemBiophysResCommun.417(1):558-63.
- 3.WillardFS,etal.Smallmoleculeallostericmodulationoftheglucagon-likePeptide-1receptorenhancestheinsulinotropiceffectofoxyntomodulin.(2012)MolPharmacol.82(6):1066-73.
- 4.NolteWM,etal.ApotentiatoroforthostericligandactivityatGLP-1Ractsviacovalentmodification.(2014)NatChemBiol.Inpress.
BETP_spec.pdf
BETP_MSDS.pdf
Productsareforresearchuseonly.Notforhumanuse
