Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemECXCR2-IN-1Cat.No.:HY-101022CASNo.:1873376-49-8分?式:C??H??Cl?FN?O?S分?量:476.35作?靶點(diǎn):CXCR作?通路:GPCR/GProtein;Immunology/Inflammation儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:5.4mg/mL(11.34mM;Needultrasonicandwarming)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.0993mL10.4965mL20.9930mL5mM0.4199mL2.0993mL4.1986mL10mM0.2099mL1.0496mL2.0993mL請(qǐng)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(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。BIOLOGICALACTIVITY?物活性CXCR2-IN-1可滲透中樞神經(jīng)系統(tǒng)的CXCR2拮抗劑，pIC50值為9.3。IC50&TargetCXCR29.3(pIC50)1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE體外研究CXCR2playsanimportantroleintheactivationandrecruitmentofneutrophilstositesofinflammation.CXCR2-IN-1(compound22)showsfavorablecentralnervoussystempenetrationproperty(Br/Bl>0.45)[1].體內(nèi)研究CXCR2-IN-1showsefficacyinacuprizone-induceddemyelinationmodelthroughoraladministration,providingevidencetosupportCXCR2tobeapotentialtherapeutictargettotreatdemyelinatingdiseasessuchasmultiplesclerosis[1].PROTOCOLAnimalMice:Micearefedwithcuprizonefor5weekstocausedemyelinatinglesionsintheCNSandthenorallyAdministration[1]administratedwithCXCR2-IN-1for9consecutivedaysatdosesof30and100mg/kgtwicedaily[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.戶(hù)使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?IntImmunopharmacol.2019Nov;76:105877?JCellMolMed.2020Sep;24(18):10604-10614.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].XuH,etal.DiscoveryofCNSPenetrantCXCR2AntagonistsforthePotentialTreatmentofCNSDemyelinatingDisorders.ACSMedChemLett.2016Feb8;7(4):397-402.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-8