HCH6-1-DataSheet-生命科學(xué)試劑-MedChemExpress

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(diǎn):FormylPeptideReceptor(FPR)作?通路:GPCR/GProtein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:250mg/mL(532.45mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.1298mL10.6489mL21.2979mL5mM0.4260mL2.1298mL4.2596mL10mM0.2130mL1.0649mL2.1298mL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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的?式助溶)1.請(qǐng)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(qǐng)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(jìng)爭(zhēng)性?肽拮抗劑。HCH6-1抑制fMLF(FPR1激動(dòng)劑)特異性激活的?中性粒細(xì)胞的趨化性、超氧離??成和彈性酶釋放。動(dòng)物實(shí)驗(yàn)中，HCH6-1對(duì)急性肺損傷(ALI)具有保護(hù)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(nèi)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(xiàn)?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