NLRP3-IN-2-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemENLRP3-IN-2Cat.No.:HY-W011082CASNo.:16673-34-0分?式:C??H??ClN?O?S分?量:368.84作?靶點(diǎn):NOD-likeReceptor(NLR)作?通路:Immunology/Inflammation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(677.80mM;Needultrasonic)H2O:<0.1mg/mL(insoluble)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.7112mL13.5560mL27.1120mL5mM0.5422mL2.7112mL5.4224mL10mM0.2711mL1.3556mL2.7112mL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，并請(qǐng)注意儲(chǔ)備液的保存?式和期限。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，配制前請(qǐng)先配制澄的儲(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，體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；以下溶劑前的百分?指該溶劑在您配制終溶液中的體積占?)：1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(5.64mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(5.64mM);Clearsolution1/2MasterofSmallMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性NLRP3-IN-2合成格列本脲的中間底物，可抑制?肌細(xì)胞中NLRP3炎癥?體的形成，在???肌缺?/再灌注后限制梗死積，且不響代謝。體內(nèi)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