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PotentdualCRTH2andprostaglandinD2(PGD2)receptorantagonist(IC50valuesare8and35nM,respectivelyinplasma).InhibitsPGD2-induceddownmodulationofCRTH2onCD16-granulocytesinhumanwholebloodaswellasPGD2-inducedcAMPresponseinplatelets.InhibitsPGD2-inducedairwayconstrictioninvivo.AlsoinhibitsBRD4(Kd=170nM).Orallybioavailable.
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
Thefollowingdataisbasedontheproductmolecularweight609.49.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
Referencesarepublicationsthatsupporttheproducts'biologicalactivity.
Liuetal(2011)DiscoveryofAMG853,aCRTH2andDPdualantagonist.ACSMed.Chem.Lett.2326PMID:24900313
Keywords:AMG853,supplier,AMG853,CRTH2,chemoattractant,receptor-homologous,molecule,expressed,on,Th4,cells,PGD2,prostaglandin,receptor,dual,antagonists,antagonism,orally,bioavailable,Prostanoid,Receptors,Prostanoid,Receptors,TocrisBioscience
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