CHPG-sodium-salt-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemECHPGsodiumsaltCat.No.:HY-101364ACASNo.:1303993-73-8分⼦式:C₈H₇ClNNaO₃分⼦量:223.59作⽤靶点:mGluR;NF-κB;ERK;Akt作⽤通路:GPCR/GProtein;NeuronalSignaling;NF-κB;MAPK/ERKPathway;StemCell/Wnt;PI3K/Akt/mTOR储存⽅式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性数据体外实验DMSO:100mg/mL(447.25mM;Needultrasonic)H2O:6.67mg/mL(29.83mM;ultrasonicandwarmingandheatto80°C)MassSolvent1mg5mg10mgConcentration制备储备液1mM4.4725mL22.3624mL44.7247mL5mM0.8945mL4.4725mL8.9449mL10mM0.4472mL2.2362mL4.4725mL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(sealedstorage,awayfrommoisture)。-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:≥2.5mg/mL(11.18mM);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%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(11.18mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(11.18mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性CHPGsodiumsalt⼀个选择性的mGluR5激动剂，并且通过TSG-6/NF-κB途径减弱BV2⼩神经胶质细胞SO2诱导的氧化应激和炎症。CHPGsodiumsalt通过ERK和Akt途径在体外和体内预防创伤性脑损伤(TBI)。IC50&TargetmGlu5NF-κBERK体外研究CHPGsodiumsalt(10-500ꢀµM;24ꢀhours)significantlyincreasesthecellviabilityanddecreasestheLDHreleaseafterSO2derivativestreatment[1].CHPGsodiumsalt(0.5ꢀmM;30ꢀmins)protectsBV2cellsagainstSO2-inducedapoptosis[1].CHPGsodiumsalt(0.5mM;30ꢀmins)treatmentaloneincreasestheexpressionofTSG-6inbothmRNAandproteinlevels[1].CellViabilityAssay[1]CellLine:BV2microglialcellsConcentration:10,50,100and500ꢀµMIncubationTime:24ꢀhoursResult:Increasedthecellviability.ApoptosisAnalysis[1]CellLine:BV2microglialcellsConcentration:0.5ꢀmMIncubationTime:30ꢀminsResult:ProtectedBV2cellsagainstSO2-inducedapoptosis.WesternBlotAnalysis[1]CellLine:BV2microglialcellsConcentration:0.5ꢀmMIncubationTime:30ꢀminsResult:IncreasedtheexpressionofTSG-6inbothmRNAandproteinlevels.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE体内研究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