ML382-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemEML382Cat.No.:HY-110285CASNo.:1646499-97-9分⼦式:C₁₈H₂₀N₂O₄S分⼦量:360.43作⽤靶点:Others作⽤通路:Others储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(277.45mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.7745mL13.8723mL27.7446mL5mM0.5549mL2.7745mL5.5489mL10mM0.2774mL1.3872mL2.7745mL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(6.94mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.94mM);ClearsolutionBIOLOGICALACTIVITY1/2MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemE⽣物活性ML382⼀种有效选择性的Mas相关G蛋⽩偶联受体X1MRGPRX1(MrgX1)正向调节剂，EC50为190nM。IC50&TargetEC50:190nM(MRGPRX1)[1]体外研究IntheabsenceofML382,theIC50forBAM8-22inhibitionofICais0.66±0.05μM.Inthepresenceof0.1μM,1μM,10μM,and30μMML382,BAM8-22IC50isreducedto0.43±0.02μM,0.25±0.02μM,0.06±0.01μM,and0.08±0.01μM,respectively.AlowerIC50generallyindicatesahigherpotency;thus,ML382dose-dependentlyincreasesthepotencyofBAM8–22,furtherdemonstratingthatML382isapositiveallostericmodulatorofMRGPRX1[1].体内研究ML382(5μM)significantlyincreasesinhibitionofICabyalowconcentrationofBAM8–22(0.5μM)inDRGneuronsfromMrgprX1mice.ML382enhancestheinhibitionofspinalsynaptictransmissionbyBAM8-22inMrgprX1mice.ML382(25μM,125μM,and250μM;5μL;i.th.;)dose-dependentlyattenuatesheathypersensitivityinMrgprX1mice.ML382(lumbarpunctureinjection;25μM,5μL)leadstoasignificantincreaseinpostconditioningtimespentintheML382-pairedchamber,comparedwiththepreconditioningvalue.ML382inhibitsnerveinjury-inducedongoingpaininMrgprX1mice[1].REFERENCES[1].LiZ,etal.TargetinghumanMas-relatedGprotein-coupledreceptorX1toinhibitpersistentpain.ProcNatlAcadSciUSA.2017;114(10):E1996-E2005.[2].WenW,etal.Discoveryandcharacterizationof2-(cyclopropanesulfonamido)-N-(2-ethoxyphenyl)benzamide,ML382:apotentandselectivepositiveallostericmodulatorofMrgX1.ChemMedChem.2015;10(1):57-61.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Fo