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蚂蚁淘在线 / 品牌中心 / Xcess / Xcessbio/BETP，GLP-1R增效剂Xcessbio Biosciences Inc/2 mg固体/M60196-2s

Xcessbio/BETP，GLP-1R增效剂Xcessbio Biosciences Inc/2 mg固体/M60196-2s

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￥2580.00
货号：M60196-2s
浏览量：127
品牌：Xcess
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ProductInformation
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. 1.SloopKW,etal.Novelsmallmoleculeglucagon-likepeptide-1receptoragoniststimulatesinsulinsecretioninrodentsandfromhumanislets.(2010)Diabetes.59(12):3099-107.
  2. 2.CheongYH,etal.Twosmallmoleculeagonistsofglucagon-likepeptide-1receptormodulatethereceptoractivationresponsedifferently.(2012)BiochemBiophysResCommun.417(1):558-63.
  3. 3.WillardFS,etal.Smallmoleculeallostericmodulationoftheglucagon-likePeptide-1receptorenhancestheinsulinotropiceffectofoxyntomodulin.(2012)MolPharmacol.82(6):1066-73.
  4. 4.NolteWM,etal.ApotentiatoroforthostericligandactivityatGLP-1Ractsviacovalentmodification.(2014)NatChemBiol.Inpress.

BETP_spec.pdf

BETP_MSDS.pdf

Productsareforresearchuseonly.Notforhumanuse

Xcess生物科学公司(XcessBio)成立于2008年,由一群顶尖的科学家来自学术界和制药/生物技术产业具有较强的专业知识在药物化学、生物化学、分子和细胞生物学。