Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemEVercirnonsodiumCat.No.:HY-15724ACASNo.:886214-18-2Synonyms:GSK-1605786sodium;CCX282-Bsodium;Traficet-ENsodium分?式:C??H??ClN?NaO?S分?量:466.91作?靶點(diǎn):CCR作?通路:GPCR/GProtein;Immunology/Inflammation儲存?式:4°C,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(storedunder

nitrogen)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:100mg/mL(214.17mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.1417mL10.7087mL21.4174mL5mM0.4283mL2.1417mL4.2835mL10mM0.2142mL1.0709mL2.1417mL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(dòng)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:5mg/mL(10.71mM);Suspendedsolution;Needultrasonic2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥5mg/mL(10.71mM);ClearsolutionBIOLOGICALACTIVITY1/2MasterofSmallMolecules—您?邊的抑制劑?師www.MedChemE?物活性Vercirnon(GSK-1605786)sodium?種具有?服活性的，選擇性的CCR9拮抗劑。Vercirnonsodium抑制CCR9介導(dǎo)的Molt-4細(xì)胞上Ca2+移動(dòng)和趨化性，IC50值分別為5.4和3.4nM。Vercirnonsodium對CCR9的選擇性?于CCR1-12和CX3CR1-7(IC50s=>10μM)。VercirnonsodiumCCR9的兩種剪接形式(CCR9A和CCR9B)的CCL25定向趨化性的等效抑制劑，IC50值分別為2.8和2.6nM。IC50&TargetCCR910nM(IC50)體外研究Vercirnon(GSK-1605786)sodiuminhibitschemotaxisofprimaryCCR9-expressingcellstoCCL25withanIC50of6.8nM.VercirnonsodiuminhibitsCCL25-InducedChemotaxisofretinoicacid(RA)-CulturedHumanTCells.VercirnonsodiuminhibitsRA-culturedcellCCL25-medidatedchemotaxisin100%humanABserumresultedinanIC50of141nM.VercirnonsodiumisapotentinhibitorofCCL25-inducedmouseandratthymocytechemotaxiswithIC50valuesof6.9nMand1.3nM,respectively[1].體內(nèi)研究Vercirnon(GSK1605786A)sodium(10,50mg/kg;s.c.;twiceperday;startingat2weeksofageuntil12weeksofage)amelioratestheseverityofintestinalinflammationintheTNFΔAREmousemodel[1].AnimalModel:C57BL/6mice(TNFΔAREMouseModelofTerminalIleitis)[1]Dosage:10,50mg/kgAdministration:Subcutaneous;twiceperday;startingat2weeksofageuntil12weeksofageResult:ResultedincompleteprotectionfromthesevereinflammationassociatedwithTNF-overexpressionat50mg/kg.Asimilarprotectiveeffectwasalsonotedwithalowerdose.REFERENCES[1].WaltersMJ,etal.CharacterizationofCCX282-B,anorallybioavailableantagonistoftheCCR9chemokinereceptor,fortreatmentofinflammatoryboweldisease.JPharmacolExpTher.2010Oct;335(1):61-9.[2].BekkerP,etal.CCR9AntagonistsintheTreatmentofUlcerativeColitis.MediatorsInflamm.2015;2015:628340.[3].ZhangJ,etal.BiarylsulfonamideCCR9inhibitorsforinflammatoryboweldisease.BioorgMedChemLett.2015Sep1;25(17):3661-4.McePdfHeightCaution:Producthasnotbeenfullyvalidatedfor