Bepotastine-tosylate-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEBepotastinetosylateCat.No.:HY-I0021ACASNo.:1160415-45-1分?式:C??H??ClN?O?S分?量:561.09作?靶點(diǎn):HistamineReceptor作?通路:GPCR/GProtein;Immunology/Inflammation;NeuronalSignaling儲(chǔ)存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性Bepotastinetosylate?種具有選擇性和?服活性的第?代組胺H1受體(histamineH1receptor)拮抗劑，可抑制組胺介導(dǎo)的神經(jīng)?長(zhǎng)因?(NGF)表達(dá)上調(diào)。Bepotastinetosylate可?于過(guò)敏性?炎，過(guò)敏性結(jié)膜炎和蕁?疹/瘙癢癥的研究。IC50&TargetHistamineH1Receptor[1][2][3][4].體外研究Bepotastinetosylate(10,100,1000μM;preincubatesfor120min)decreasesthereleaseofhistamineinducedbyA23187treatment,whichreachesastatisticallysignificantreduceslevelat1000μM[1].Bepotastinetosylate(50μM;1h)suppressestheexpressionofNGFmRNAinNHEKs[2].CellViabilityAssay[1]CellLine:RPMCsConcentration:10,100,1000μMIncubationTime:120min(preincubate)Result:Decreasedthereleaseofhistamine.WesternBlotAnalysis[2]CellLine:NHEKs1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEConcentration:50μM(preincubation)IncubationTime:1hResult:SuppressedtheexpressionofNGFmRNAinNHEKs.體內(nèi)研究Bepotastinetosylate(10g/L;eyedrop;3timesatintervalsof20mininoneeye)demonstratessignificantinhibitionofPAF-inducedconjunctivaleosinophilinfiltration[1].Bepotastinetosylate(3mg/kg;p.o.;once)suppressesscratchingbehaviortoafrequencyof59.0andadurationof14.57seconds,whicharealmostthesamelevelscompareswiththecontrol[3].Bepotastinetosylate(10mg/kg;p.o.;once)significantlysuppressesserumLTB4levelsto711.3pg/mLat1hand858.8pg/mLat2hinNC/Ngamicewitharash[3].AnimalModel:Guineapigs(6-week-old)[1].Dosage:10g/L(1.0%(w/v))for10μL.Administration:Eyedrop;3timesatintervalsof20min(inoneeye)Result:InhibitedPAF-inducedconjunctivaleosinophilinfiltration.AnimalModel:MaleBALB/cmice(12-week-old);NC/Ngamice[3].Dosage:3,10mg/kgAdministration:Oraladministration;once(1hbeforeinducesscratchingbehaviorofMaleBALB/cmice).Result:Significantlyinhibitedhistamine-mediatedscratchingbehaviorinmaleBALB/cmice.SignificantlysuppressedserumLTB4levelsinNC/Ngamicewitharash.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?JMedChem.2021Feb23.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].JonIWilliams,etal.Non-clinicalpharmacology,pharmacokinetics,andsafetyfindingsfortheantihistaminebepotastinebesilate.CurrMedResOpin.2010Oct;26(10):2329-38.[2].KidaT,etal.Bepotastinebesilate,ahighlyselectivehistamineH(1)receptorantagonist,suppressesvascularhyperpermeabilityandeosinophilrecruitmentininvitroandinvivoexperimentalallergicconjunctivitismodels.ExpEyeRes.2010Jul;91(1):85-91.[3].TanizakiH,etal.OraladministrationofbepotastinebesilatesuppressedscratchingbehaviorofatopicdermatitismodelNC/Ngamice.IntArchAllergyImmunol.2008;145(4):277-82.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE[4].KamataY,etal.Bepotastinebesilatedownregulatestheexpressionofnerveelongationfactorsinnormalhumanepidermalkeratinocytes.JDermatolSci.2018Apr23:S0923-1811(18)30186-5.McePdfHeightCaution:Producthasnotbeenfull