Pamapimod-Ro4402257-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEPamapimodCat.No.:HY-10405CASNo.:449811-01-2Synonyms:Ro4402257;R1503分⼦式:C₁₉H₂₀F₂N₄O₄分⼦量:406.38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DMSO:≥34mg/mL(83.67mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM2.4608mL12.3038mL24.6075mL5mM0.4922mL2.4608mL4.9215mL10mM0.2461mL1.2304mL2.4608mL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。BIOLOGICALACTIVITY⽣物活性Pamapimod(Ro4402257)⼀种有效的，选择性和⼝服活性的p38MAPK抑制剂，对于p38α和p38β的IC50分别为14nM和480nM，Ki分别为1.3nM和120nM。Pamapimod对p38δ或p38γ亚型没有活性1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE。Pamapimod可⽤于类风湿关节炎和其他⾃⾝免疫性疾病的研究。IC50&Targetp38αp38αp38βp38β14nM(IC50)1.3nM(Ki)480(IC50)120nM(Ki)体外研究PamapimodbindstoJNKkinaseswithKivaluesof190nM,16nMand19nMforJnk1,Jnk2andJnk3,respectively[1].Afterlipopolysaccharide(LPS)stimulationofthehumanmyelomonocyticcellline(THP-1),secretionofTNF-αisinhibitedbyPamapimod,withanEC50of25nM.PamapimodsuppressesTNF-αandIL-1βproductioninwholeblood,withEC50valuesof0.40and0.10μM,respectively[1].体内研究Pamapimod(0-150mg/kg;oralgavage;oncedaily;DBA/1Jfemalemice)treatmentreducesinflammationandbonelossinmurinecollagen-inducedarthritis[1].AnimalModel:DBA/1Jfemalemice(8-10weeksofage)inducedmurinecollagen[1]Dosage:0mg/kg,3mg/kg,10mg/kg,30mg/kg,90mg/kg,150mg/kgAdministration:Oralgavage;oncedailyResult:Reducedinflammationandboneloss.REFERENCES[1].Hill,R.J.etal.Pamapimod,anovelp38mitogen-activatedproteinkinaseinhibitor:preclinicalanalysisofefficacyandselectivity.TheJournalofpharmacologyandexperimentaltherapeutics327,610-619,doi:10.1124/jpet.108.139006(2008).McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Te