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HighaffinityandselectiveGPERreceptorantagonist(Ki=20nM)thatdisplaysnoaffinityforERαandERβatconcentrationsupto10μM.Inhibitsagonist-inducedcalciummobilizationinvitro(EC50of~185nM)andantagonizestheantidepressiveandrenoprotectiveeffectsofestrogeninvivo.
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
Thefollowingdataisbasedontheproductmolecularweight370.24.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
Referencesarepublicationsthatsupporttheproducts'biologicalactivity.
Dennisetal(2009)InvivoeffectsofaGPR30antagonist.Nat.Chem.Biol.5421PMID:19430488
Hutchensetal(2012)Estrogenprotectsrenalendothelialbarrierfunctionfromischemia-reperfusioninvitroandinvivo.Am.J.Physiol.RenalPhysiol.303377PMID:22622457
Keywords:G-15,supplier,high,affinity,selective,GPR30,antagonist,estrogen,oestrogen,receptors,GPER,Estrogen,(GPER),Receptors,Estrogen,(GPER),Receptors,TocrisBioscience
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