ML382-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemEML382Cat.No.:HY-110285CASNo.:1646499-97-9分?式:C??H??N?O?S分?量:360.43作?靶點:Others作?通路:Others儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:100mg/mL(277.45mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.7745mL13.8723mL27.7446mL5mM0.5549mL2.7745mL5.5489mL10mM0.2774mL1.3872mL2.7745mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存?式和期限。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當(dāng)?shù)娜芙?案，配制前請先配制澄的儲備液，再依次添加助溶劑(為保證實驗結(jié)果的可靠性，體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；澄的儲備液可以根據(jù)儲存條件，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.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(6.94mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.94mM);ClearsolutionBIOLOGICALACTIVITY1/2MasterofSmallMolecules—您?邊的抑制劑?師www.MedChemE?物活性ML382?種有效選擇性的Mas相關(guān)G蛋?偶聯(lián)受體X1MRGPRX1(MrgX1)正向調(diào)節(jié)劑，EC50為190nM。IC50&TargetEC50:190nM(MRGPRX1)[1]體外研究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].體內(nèi)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