Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemEEmedastineCat.No.:HY-108411CASNo.:87233-61-2分?式:C??H??N?O分?量:302.41作?靶點(diǎn):HistamineReceptor作?通路:GPCR/GProtein;Immunology/Inflammation;NeuronalSignaling儲存?式:Pureform-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:125mg/mL(413.35mM;Needultrasonic)Ethanol:100mg/mL(330.68mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM3.3068mL16.5338mL33.0677mL5mM0.6614mL3.3068mL6.6135mL10mM0.3307mL1.6534mL3.3068mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存?式和期限。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動物和給藥?式選擇適當(dāng)?shù)娜芙?案，配制前請先配制澄的儲備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；以下溶劑前的百分?指該溶劑在您配制終溶液中的體積占?)：1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(6.88mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(6.88mM);Clearsolution1/2MasterofSmallMolecules—您?邊的抑制劑?師www.MedChemE3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(6.88mM);ClearsolutionBIOLOGICALACTIVITY?物活性Emedastine?種具有?服活性，選擇性和?親和?的組胺H1受體拮抗劑，Ki值為1.3nM。Emedastine是?種苯并咪唑衍?物，具有強(qiáng)?的抗過敏特性，可?于過敏性?炎，過敏性?膚疾病和過敏性結(jié)膜炎。IC50&TargetH1ReceptorH2ReceptorH3Receptor1.3nM(Ki)49067nM(Ki)12430nM(Ki)體外研究EmedastineinhibitshistamineH2receptor(Ki=49067nM)andhistamineH3receptor(Ki=12430nM)[1].HighconcentrationsofEmedastine(1and10ng/ml)significantlyinhibitstype1collagenproductioninnormalhumandermalfibroblasts[2].Emedastine(1,10,100,1000nM)atconcentrationsof≥10nMinhibitsCCchemokine-elicitedeosinophilmigration[2].體內(nèi)研究Emedastine(0.03,0.1,0.3mg/kg;orally;pretreatmentof30min)significantlysuppresseshistamine-inducedscratchingwith0.1and0.3mg/kgbutnot0.03mg/kg[3].PretreatmentwithEmedastine(0.03,0.1,0.3mg/kg;orally)significantlyinhibitsthescratchinginducedbysubstancePandleukotrieneB[3].Emedastine(0.3mg/kg,p.o.)producessignificantinhibitionofpassiveperitonealanaphylaxisinguinea-pigs[2].Emedastineinhibitshistamine-inducedcontractionsofisolatedileum(IC50=6.1nM)[2].AnimalModel:MaleICRmice5-6weeksofage[3]Dosage:0.03,0.1,0.3mg/kgAdministration:Orally;30minbeforepruritogeninjectionResult:Significantlysuppressedhistamine-inducedscratchingwithpretreatmentof0.1and0.3mg/kg.REFERENCES[1].SharifNA,etal.Emedastine:apotent,highaffinityhistamineH1-receptor-selectiveantagonistforocularuse:receptorbindingandsecondmessengerstudies.JOculPharmacol.1994Winter;10(4):653-64.[2].MurotaH,etal.Emedastinedifumarate:areviewofitspotentialamelioratingeffectfortissueremodelinginallergicdiseases.ExpertOpinPharmacother.2009Aug;10(11):1859-67.[3].AndohT,etal.InvolvementofblockadeofleukotrieneB(4)actioninanti-pruriticeffectsofemedastineinmice.EurJPharmacol.2000Oct6;406(1):149-52.McePdfHeight2/2MasterofSmallMolecules—您?邊的抑制劑?師www.MedChemECaution:Producthasnotbeenfullyvalida