Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPamapimodCat.No.:HY-10405CASNo.:449811-01-2Synonyms:Ro4402257;R1503分?式:C??H??F?N?O?分?量:406.38作?靶點(diǎn):p38MAPK;Autophagy作?通路:MAPK/ERKPathway;Autophagy儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:≥34mg/mL(83.67mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.4608mL12.3038mL24.6075mL5mM0.4922mL2.4608mL4.9215mL10mM0.2461mL1.2304mL2.4608mL請(qǐng)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(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。BIOLOGICALACTIVITY?物活性Pamapimod(Ro4402257)?種有效的，選擇性和?服活性的p38MAPK抑制劑，對(duì)于p38α和p38β的IC50分別為14nM和480nM，Ki分別為1.3nM和120nM。Pamapimod對(duì)p38δ或p38γ亞型沒有活性1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE。Pamapimod可?于類風(fēng)濕關(guān)節(jié)炎和其他??免疫性疾病的研究。IC50&Targetp38αp38αp38βp38β14nM(IC50)1.3nM(Ki)480(IC50)120nM(Ki)體外研究PamapimodbindstoJNKkinaseswithKivaluesof190nM,16nMand19nMforJnk1,Jnk2andJnk3,respectively[1].Afterlipopolysaccharide(LPS)stimulationofthehumanmyelomonocyticcellline(THP-1),secretionofTNF-αisinhibitedbyPamapimod,withanEC50of25nM.PamapimodsuppressesTNF-αandIL-1βproductioninwholeblood,withEC50valuesof0.40and0.10μM,respectively[1].體內(nèi)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