Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemECHPGsodiumsaltCat.No.:HY-101364ACASNo.:1303993-73-8分?式:C?H?ClNNaO?分?量:223.59作?靶點(diǎn):mGluR;NF-κB;ERK;Akt作?通路:GPCR/GProtein;NeuronalSignaling;NF-κB;MAPK/ERKPathway;StemCell/Wnt;PI3K/Akt/mTOR儲存?式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:100mg/mL(447.25mM;Needultrasonic)H2O:6.67mg/mL(29.83mM;ultrasonicandwarmingandheatto80°C)MassSolvent1mg5mg10mgConcentration制備儲備液1mM4.4725mL22.3624mL44.7247mL5mM0.8945mL4.4725mL8.9449mL10mM0.4472mL2.2362mL4.4725mL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(fù)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(sealedstorage,awayfrommoisture)。-80°C儲存時，請?jiān)?個?內(nèi)使?，-20°C儲存時，請?jiān)?個?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動物和給藥?式選擇適當(dāng)?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(shí)驗(yàn)結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，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.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(11.18mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(11.18mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(11.18mM);ClearsolutionBIOLOGICALACTIVITY?物活性CHPGsodiumsalt?個選擇性的mGluR5激動劑，并且通過TSG-6/NF-κB途徑減弱BV2?神經(jīng)膠質(zhì)細(xì)胞SO2誘導(dǎo)的氧化應(yīng)激和炎癥。CHPGsodiumsalt通過ERK和Akt途徑在體外和體內(nèi)預(yù)防創(chuàng)傷性腦損傷(TBI)。IC50&TargetmGlu5NF-κBERK體外研究CHPGsodiumsalt(10-500?μM;24?hours)significantlyincreasesthecellviabilityanddecreasestheLDHreleaseafterSO2derivativestreatment[1].CHPGsodiumsalt(0.5?mM;30?mins)protectsBV2cellsagainstSO2-inducedapoptosis[1].CHPGsodiumsalt(0.5mM;30?mins)treatmentaloneincreasestheexpressionofTSG-6inbothmRNAandproteinlevels[1].CellViabilityAssay[1]CellLine:BV2microglialcellsConcentration:10,50,100and500?μMIncubationTime:24?hoursResult:Increasedthecellviability.ApoptosisAnalysis[1]CellLine:BV2microglialcellsConcentration:0.5?mMIncubationTime:30?minsResult:ProtectedBV2cellsagainstSO2-inducedapoptosis.WesternBlotAnalysis[1]CellLine:BV2microglialcellsConcentration:0.5?mMIncubationTime:30?minsResult:IncreasedtheexpressionofTSG-6inbothmRNAandproteinlevels.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE體內(nèi)研究CHPGsodiumsalt(injection;250nM;for7days)reducessignificantlycerebrallesionvolume[2].AnimalModel:AdultSprague-Dawleymaleratsweighing280-320g[2]Dosage:250nMAdministration:Injection;for7daysResult:Reducedsignificantlycerebrallesionvolume.REFERENCES[1].QiuJL,etal.TheselectivemGluR5agonistCHPGattenuatesSO-inducedoxidativestressandinflammationthroughTSG-6/NF-κBpathwayinBV2microglialcells.NeurochemInt.2015Jun-Jul;85-86:46-52.[2].ChenT,etal.TheselectivemGluR5agonistCHPGprotectsagainsttraumaticbraininjuryinvitroandinvivoviaERKandAktpathway.IntJMolMed.2012Apr;29(4):630-6.McePdfHeightCaution:Producthasnotbeenfullyvali