HCH6-1-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEHCH6-1Cat.No.:HY-101283CASNo.:1435265-06-7分⼦式:C₂₈H₂₇N₃O₄分⼦量:469.53作⽤靶点:FormylPeptideReceptor(FPR)作⽤通路:GPCR/GProtein储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:250mg/mL(532.45mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.1298mL10.6489mL21.2979mL5mM0.4260mL2.1298mL4.2596mL10mM0.2130mL1.0649mL2.1298mL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>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(4.43mM);Clearsolution1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.43mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性HCH6-1⼀种有效的甲酰肽受体1(FPR1)的竞争性⼆肽拮抗剂。HCH6-1抑制fMLF(FPR1激动剂)特异性激活的⼈中性粒细胞的趋化性、超氧离⼦⽣成和弹性酶释放。动物实验中，HCH6-1对急性肺损伤(ALI)具有保护作⽤，可⽤于FPR1参与的炎症性肺部疾病的研究。IC50&TargetIC50:Formylpeptidereceptor1(FPR1)[1]体外研究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].体内研究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.户使⽤本产品发表的科研⽂献•CancerRes.2022Aug16;82(16):2887-2903.Seemorecustomervalidationsonwww.MedChemEREFERENCES2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[1].YangSC,etal.DipeptideHCH6-1inhibitsneutrophilactivationandprotectsagainstacutelunginjurybyblockingFPR1.FreeRadicBiolMed.2017May;106:254-269McePdfHeightCaution:Producthasnotbeenfullyva