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CaSRbiasedallostericmodulator(pEC50=7.8-8.1).Calcimimetic.DisplaysABIlitytobiassignallingtowardstheaccumulationofPERK1/2andIP1.Reducesparathyroidhormone(PTH)levelsinratserumwithoutinducingthereleaseofcalcitonin.ExhibitsnosignificantactivationofhumanGABABortypeIPTHreceptors.Orallyactive.
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
Thefollowingdataisbasedontheproductmolecularweight283.39.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
Referencesarepublicationsthatsupporttheproducts'biologicalactivity.
Cooketal(2015)BiasedallostericmodulationattheCaSreceptorengenderedbystructurallydiversecalcimimetics.Br.J.Pharmacol.172185PMID:25220431
Maetal(2011)CharacterizationofhighlyefficaciousallostericagoNISTsofthehumancalcium-sensingreceptor.J.Pharmacol.Exp.Ther.337275PMID:21239511
Leachetal(2016)Towardsastructuralunderstandingofallostericdrugsatthehumancalcium-sensingreceptor.Cell.Res.26574PMID:27002221
Keywords:AC265347,supplier,AC265347,CaSR,biased,allosteric,modulator,calcimimetic,parathyroid,homrone,PTH,calcitonin,PERK1/2,IP1,accumulation,orally,active,Calcium-Sensing,Receptor,Calcium-Sensing,Receptor,TocrisBioscience
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