LMT-28-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemELMT-28Cat.No.:HY-102084CASNo.:1239600-18-0分⼦式:C₁₇H₂₉NO₄分⼦量:311.42作⽤靶点:InterleukinRelated作⽤通路:Immunology/Inflammation储存⽅式:Pureform-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(321.11mM;Needultrasonic)H2O:<0.1mg/mL(insoluble)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.2111mL16.0555mL32.1110mL5mM0.6422mL3.2111mL6.4222mL10mM0.3211mL1.6055mL3.2111mL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:2.5mg/mL(8.03mM);Suspendedsolution;Needultrasonic2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.5mg/mL(8.03mM);Suspendedsolution;Needultrasonic3.请依序添加每种溶剂：10%DMSO>>90%cornoil1/3MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(8.03mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性LMT-28⼀种具有⼝服活性的通过直接与gp130结合⽽发挥作⽤的IL-6抑制剂。LMT-28具有低毒性，并选择性抑制IL-6诱导的STAT3、JAK2和gp130的磷酸化。IC50&TargetIL-6体外研究LMT-28reducesIL-6-inducedluciferaseactivityby~90%ataconcentrationof50μMandexhibitsanIC50valueof5.9μM.LMT-28(1-10μM;72hours)inhibitsIL-6-inducedproliferationofthehumanerythroleukemiccelllineTF-1[1].LMT-28(1-100μM;1hour)selectivelyinhibitsIL-6-inducedphosphorylationofSTAT3,JAK2,andgp130[1].CellProliferationAssay[1]CellLine:TF-1cells(1ng/mLIL-6-induced)Concentration:1,10,100,1000,10000nMIncubationTime:72hoursResult:MarkedlyinhibitedIL-6–inducedTF-1proliferationwithanIC50valueof7.5μM.WesternBlotAnalysis[1]CellLine:HepG2cells(treatedwith10ng/mLIL-6)Concentration:1,3,10,30,and100μMIncubationTime:1hourResult:InhibitsIL-6-inducedphosphorylationofSTAT3,JAK2,andgp130.体内研究LMT-28(0-0.5mg/kg;p.o.;oncedailyfor15days)alleviatesCIAinmice[1].LMT-28(0.25or1mg/kg;p.o.)amelioratestheprogressionofpancreatitisinmice.LMT-28bindsdirectlyandspecificallytogp130,andtherebyinhibitstheinteractionofgp130withtheIL-6/IL-6Rαcomplex[1].AnimalModel:Six-week-oldmaleDBA/1Jmice(collagen-inducedarthritismice,CIA)[1]Dosage:0-0.5mg/kgAdministration:Oral;oncedailyfor15daysResult:Markedlyreducedtheserumlevelsofcartilageoligomericmatrixprotein(COMP)by50%,serumamyloidP(SAP)by55%,andanti-CIIIgGby62%.2/3MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemEREFERENCES[1].HongSS,etal.ANovelSmall-Molecule