Losmapimod-GSK-AHAB-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemELosmapimodCat.No.:HY-10402CASNo.:585543-15-3Synonyms:GSK-AHAB;GW856553X;SB856553分⼦式:C₂₂H₂₆FN₃O₂分⼦量:383.46作⽤靶点:p38MAPK;Autophagy作⽤通路:MAPK/ERKPathway;Autophagy储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验Ethanol:33.33mg/mL(86.92mM;Needultrasonic)DMSO:27.5mg/mL(71.72mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.6078mL13.0392mL26.0783mL5mM0.5216mL2.6078mL5.2157mL10mM0.2608mL1.3039mL2.6078mL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；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。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。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:2.75mg/mL(7.17mM);Suspendedsolution;Needultrasonic2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.75mg/mL(7.17mM);Suspendedsolution;Needultrasonic3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.75mg/mL(7.17mM);Clearsolution4.请依序添加每种溶剂：10%EtOH>>90%(20%SBE-β-CDinsaline)Solubility:2.5mg/mL(6.52mM);Suspendedsolution;Needultrasonic5.请依序添加每种溶剂：10%EtOH>>90%cornoilSolubility:≥2.5mg/mL(6.52mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Losmapimod(GSK-AHAB)⼀种有效的，具有⼝服活性的选择性p38MAPK抑制剂，抑制p38α和p38β的pKi值分别为8.1和7.6[1]。IC50&TargetpKi:8.1(p38α),7.6(p38β)体内研究Inthespontaneouslyhypertensivestroke-pronerat(SHR-SP),chronictreatmentwithGSK-AHABsignificantlyanddose-dependentlyimprovessurvival,endothelial-dependentand-independentvascularrelaxation,andindicesofrenalfunction,anditattenuatesdyslipidemia,hypertension,cardiacremodeling,plasmareninactivity(PRA),aldosterone,andinterleukin-1β(IL-1β)[1].PROTOCOLAnimalMaleSHR-SPs(n=70)arerandomlyassignedaccordingtobodyweightintofivegroups(n=14pergroup):Administration[1]normaldietcontrols(ND),highsalt-fatdietcontrols(SFD),SFD+GSK-AHAB(1.2mg/kg/day),andSFD+GSK-AHAB(12mg/kg/day)andSFD+MK966(18mg/kg/day).AlldrugsareadministeredinthedietbymixingwiththeSFD.Asubgroupofanimalsfromeachgroup(n=6pergroup)areanesthetizedandsurgicallyinstrumentedwithradiotelemetryunitsfortheconsciousmeasurementofmeanarterialbloodpressureandheartrate.Theseanimalsareallowedtorecoverforatleast7daysbeforethestartofthestudy.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•EBioMedicine.2018Feb;28:51-61.•CellSyst.2018Apr25;6(4):424-443.e7.•CellMolLifeSci.2022Aug5;79(8):467.•Aging(AlbanyNY).2021Aug10;13(15):19088-19107.•AmJPhysiolLungCellMolPhysiol.2012Nov15;303(10):L929-38.Seemorecustomervalidationsonwww.MedChemE2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEREFERENCES[1].WilletteRN,etal.Differentialeffectsofp38mitogen-activatedproteinkinaseandcyclooxygenase2inhibitorsinamodelofcardiovasculardisease.JPharmacolExpTher.2009Sep;330(3):964-70.[2].ZhangXM,etal.Suppressionofmitochondrialfissioninexperimentalcerebralischemia:Thepotentialneuroprotectivetargetofp38MAPKinhibition.NeurochemInt.2015Nov;90:1-8.McePdfHeightCaution:Producthas