CXCR2-IN-2-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemECXCR2-IN-2Cat.No.:HY-120878CASNo.:1838123-21-9分?式:C??H??ClN?O?S分?量:414.9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:240mg/mL(578.45mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.4102mL12.0511mL24.1022mL5mM0.4820mL2.4102mL4.8204mL10mM0.2410mL1.2051mL2.4102mL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?。體內(nèi)實(shí)驗(yàn)請(qǐng)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。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥6mg/mL(14.46mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性CXCR2-IN-2?種選擇性的，可穿過?腦屏障的，具有?服?物利?的CXCR2拮抗劑(在β-arrestin和CXCR2Tango實(shí)驗(yàn)中，IC50分別為5.2nM/1nM)。CXCR2-IN-2?CXCR1具有~730倍的選擇性，?所有其他趨化因?受體的選擇性?于1900倍。CXCR2-IN-2抑制?全?Gro-α誘導(dǎo)的CD11b表達(dá)，IC50值為0.04μM。IC50&TargetCXCR2CXCR15.2nM(IC50)3.8μM(IC50)體內(nèi)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.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?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