Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEHCH6-1Cat.No.:HY-101283CASNo.:1435265-06-7分?式:C??H??N?O?分?量:469.53作?靶點:FormylPeptideReceptor(FPR)作?通路:GPCR/GProtein儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:250mg/mL(532.45mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.1298mL10.6489mL21.2979mL5mM0.4260mL2.1298mL4.2596mL10mM0.2130mL1.0649mL2.1298mL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；?旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內使?，-20°C儲存時，請在1個?內使?。體內實驗請根據(jù)您的實驗動物和給藥?式選擇適當?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當保存；體內實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；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.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(4.43mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.43mM);ClearsolutionBIOLOGICALACTIVITY?物活性HCH6-1?種有效的甲酰肽受體1(FPR1)的競爭性?肽拮抗劑。HCH6-1抑制fMLF(FPR1激動劑)特異性激活的?中性粒細胞的趨化性、超氧離??成和彈性酶釋放。動物實驗中，HCH6-1對急性肺損傷(ALI)具有保護作?，可?于FPR1參與的炎癥性肺部疾病的研究。IC50&TargetIC50:Formylpeptidereceptor1(FPR1)[1]體外研究Inacell-impermeablecytochromecreductionassay,HCH6-1significantlyinhibitssuperoxideaniongenerationinfMLF(FPR1agonist)-activatedneutrophilswithanIC50of0.32μM.HCH6-1hasfewerinhibitoryeffectsinWKYMVm(dualFPR1/FPR2agonist)-andMMK1(FPR2agonist)-activatedneutrophils,withIC50sof4.98±0.27μMand17.68±2.77μM,respectively[1].HCH6-1doesnotinduceLDHreleaseevenat30μM,soitdoesnothavecytotoxiceffectsinhumanneutrophils.HCH6-1doesnotalterthelevelofxanthine/xanthineoxidasesuperoxideanionandDPPHradicalincell-freesystems[1].HCH6-1significantlyinhibitselastasereleaseinfMLF-activatedneutrophils,withanIC50of0.57μM.However,inneutrophilstriggeredbyWKYMVmorMMK1,HCH6-1inhibitselastasereleaseathigherconcentrations,withIC50sof5.22±0.69μMand10.00±0.65μM,respectively[1].體內研究HCH6-1(intraperitonealinjection;50mg/kg;1hbeforeLPSsprayor30minafterLPSspray)alonedoesnotinduceairspaceinflammation.HCH6-1pretreatmentreducesinflammatorycellinfiltrationanddistortionofpulmonaryarchitectureinthepresenceofLPS.HCH6-1posttreatmentshowsinhibitoryeffectsonneutrophilaccumulationandlungdamageinLPS-inducedALImice[1].AnimalModel:C57BL/6mice(20-25g,7-8weeksold)[1]Dosage:50mg/kgAdministration:Intraperitonealinjection;50mg/kg;1hbeforeLPSsprayor30minafterLPSsprayResult:AmelioratedALIinLPS-inducedmice.HCH6-1-mediateddecreasingofneutrophilrecruitmentservesasaprotectivemechanisminALImice.戶使?本產(chǎn)品發(fā)表的科研?獻?CancerRes.2022Aug16;82(16):2887-2903.Seemorecustomervalidationsonwww.MedChemEREFERENCES2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE[1].YangSC,etal.DipeptideHCH6-1inhibitsneutrophilactivationandprotectsagainstacutelunginjurybyblockingFPR1.FreeRadicBiolMed.2017May;106:254-269McePdfHeightCaution:Producthasnotbeenfullyva