Olcegepant-Standard-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemEOlcegepant(Standard)Cat.No.:HY-10095RCASNo.:204697-65-4分子式:C₃₈H₄₇Br₂N₉O₅分子量:869.65作用靶点:CGRPReceptor;ReferenceStandards作用通路:GPCR/GProtein;NeuronalSignaling;Others储存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性Olcegepant(Standard)是Olcegepant(HY-10095)的分析标准品。本产品用于研究及分析应用。Olcegepant(BIBN-4096)是有效和选择性的降钙素基因相关肽1(CGRP1)受体拮抗剂，IC50和Ki分别为0.03nM，14.4pM[1][2]。IC50&TargetIC50:0.03nM(CGRP1)[1]Ki:14.4pM(hCGRP)[2]REFERENCESRudolfK,etal.Developmentofhumancalcitoningene-relatedpeptide(CGRP)receptorantagonists.1.PotentandselectivesmallmoleculeCGRPantagonists.1-[N2-[3,5-dibromo-N-[[4-(3,4-dihydro-2(1H)-oxoquinazolin-3-yl)-1-piperidinyl]carbonyl]-D-tyrosyl]-l-lysyl]-4-(4-pyridinyl)piperazine:thefirstCGRPantagonistforclinicaltrialsinacutemigraine.JMedChem.2005Sep22;48(19):5921-31.DoodsH,etal.PharmacologicalprofileofBIBN4096BS,thefirstselectivesmallmoleculeCGRPantagonist.BrJPharmacol.2000Feb;129(3):420-3.EdvinssonL,etal.EffectoftheCGRPreceptorantagonistBIBN4096BSinhumancerebral,coronaryandomentalarteriesandinSK-N-MCcells.EurJPharmacol.2002Jan2;434(1-2):49-53.SixtML,etal.Calcitoningene-relatedpeptidereceptorantagonistOlcegepantactsinthespinaltrigeminalnucleus.Brain.2009Nov;132(Pt11):3134-41.MichotB,etal.Differentialeffectsofcalcitoningene-relatedpeptidereceptorblockadebyOlcegepantonmechanicalallodyniainducedbyligationoftheinfraorbitalnervevsthesciaticnerveintherat.Pain.2012Sep;153(9):1939-48.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792;0