CXCR2-IN-2-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemECXCR2-IN-2Cat.No.:HY-120878CASNo.:1838123-21-9分⼦式:C₁₈H₂₃ClN₂O₅S分⼦量:414.9作⽤靶点:CXCR作⽤通路:GPCR/GProtein;Immunology/Inflammation储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:240mg/mL(578.45mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.4102mL12.0511mL24.1022mL5mM0.4820mL2.4102mL4.8204mL10mM0.2410mL1.2051mL2.4102mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥6mg/mL(14.46mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性CXCR2-IN-2⼀种选择性的，可穿过⾎脑屏障的，具有⼝服⽣物利⽤的CXCR2拮抗剂(在β-arrestin和CXCR2Tango实验中，IC50分别为5.2nM/1nM)。CXCR2-IN-2⽐CXCR1具有~730倍的选择性，⽐所有其他趋化因⼦受体的选择性⼤于1900倍。CXCR2-IN-2抑制⼈全⾎Gro-α诱导的CD11b表达，IC50值为0.04μM。IC50&TargetCXCR2CXCR15.2nM(IC50)3.8μM(IC50)体内研究CXCR2-IN-2(compound68)(1-10mg/kg;p.o.;twicedailyfor3days)dose-dependentlyreducesneutrophilinfiltrationinvivoinratandmouseairpouchmodels[1].AnimalModel:6-8weekoldmaleC57Bl/6mice(AirPouchModelinMouse)[1]Dosage:1,3,and10mg/kgAdministration:P.o.;twicedailyfor3daysResult:Significantlyinhibitedneutrophilinfiltrationintomouseairpouch.AnimalModel:8-10weekoldmaleWistarrats(AirPouchModelinRat)[1]Dosage:1,3,and10mg/kgAdministration:P.o.;twicedailyfor3daysResult:Inhibitedneutrophilmigrationtoairpouchinrat.户使⽤本产品发表的科研⽂献•JInflammRes.2021Apr12;14:1375-1385.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].LuH,etal.DiscoveryofNovel1-Cyclopentenyl-3-phenylureasasSelective,BrainPenetrant,andOrallyBioavailableCXCR2Antagonists.JMedChem.2018;61(6):2518-2532.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly