NLRP3-IN-2-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemENLRP3-IN-2Cat.No.:HY-W011082CASNo.:16673-34-0分⼦式:C₁₆H₁₇ClN₂O₄S分⼦量:368.84作⽤靶点:NOD-likeReceptor(NLR)作⽤通路:Immunology/Inflammation储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:250mg/mL(677.80mM;Needultrasonic)H2O:<0.1mg/mL(insoluble)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.7112mL13.5560mL27.1120mL5mM0.5422mL2.7112mL5.4224mL10mM0.2711mL1.3556mL2.7112mL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，并请注意储备液的保存⽅式和期限。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，配制前请先配制澄的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的⼯作液，建议您现⽤现配，当天使⽤；澄的储备液可以根据储存条件，适当保存；以下溶剂前的百分⽐指该溶剂在您配制终溶液中的体积占⽐)：1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(5.64mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(5.64mM);Clearsolution1/2MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性NLRP3-IN-2合成格列本脲的中间底物，可抑制⼼肌细胞中NLRP3炎症⼩体的形成，在⼩⿏⼼肌缺⾎/再灌注后限制梗死积，且不响代谢。体内研究NLRP3-IN-2iswelltoleratedwithnoeffectsontheglucoselevelsinvivo[1].NLRP3-IN-2(100mg/kg)treatmentinamodelofAMIduetoischemia+reperfusionsignificantlyinhibitstheactivityofinflammasome(caspase-1)intheheartby90%(P40%,P70%,P[1].AnimalModel:Experimentalacutemyocardialinfarction(AMI)modelinmice[1].Dosage:100mg/kg.Administration:Intraperitonealadministration30minutespriortosurgery,thenevery6hoursfor3additionaldoses.Result:Ledtoasignificant>90%reductionincaspase-1activity(reflectiveoftheformationofanactiveinflammasome)inthehearttissuemeasured24hoursafterischemia.LedtoasignificantreductionintheinfarctsizemeasuredwithTTC(>40%reduction)ortroponinIlevels(>70%reduction)whencomparedwithvehiclealone.REFERENCES[1].CarloMarchetti,etal.AnovelpharmacologicinhibitoroftheNLRP3inflammasomelimitsmyocardialinjuryafterischemia-reperfusioninthemouse.JCardiovascPharmacol.2014Apr;63(4):316-322.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonl