BMS-582949-hydrochloride-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEBMS-582949hydrochlorideCat.No.:HY-14305ACASNo.:912806-16-7分⼦式:C₂₂H₂₇ClN₆O₂分⼦量:442.94作⽤靶点:p38MAPK;Autophagy作⽤通路:MAPK/ERKPathway;Autophagy储存⽅式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性数据体外实验DMSO:25mg/mL(56.44mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.2576mL11.2882mL22.5764mL5mM0.4515mL2.2576mL4.5153mL10mM0.2258mL1.1288mL2.2576mL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(sealedstorage,awayfrommoisture)。-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.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.64mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性BMS-582949hydrochloride具有⼝服活性的、⾼度选择性的p38αMAPK抑制剂，其IC50值为13nM。BMS-582949hydrochloride具有明显改的药代动⼒学特征，能⽤于炎症性疾病的研究。IC50&Targetp38αMAPKTNFα13nM(IC50)50nM(IC50,incells)体外研究BMS-582949displaysap38αIC50of13nMandacellularTNFαIC50of50nM[1].BMS-582949isaweakinhibitorofCYP3A4BMS-582949displays>2000-foldselectivityforp38αoveradiversepanelof57kinasesthatincludeserinekinases,nonreceptortyrosinekinases,receptortyrosinekinases,andthep38γandδisoforms[1].体内研究BMS-582949(5-100mg/kg,orally)iseffectiveinboththeacutemurinemodelofinflammationandratadjuvantarthritismodeldespiteitsslightlyreducedpotency[1].AnimalModel:MaleSprague-Dawleyrats(250-300g)adjuvantarthritismodel[1].Dosage:1,10,100mg/kg.Administration:Orallyoncedaily(fromday11today19).Result:Displayeddose-dependentreductioninpawswellingwithqddosing,withefficacyobservedatdosesof10and100mg/kg.户使⽤本产品发表的科研⽂献•OncolRes.2021Feb11.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].LiuC,etal.Discoveryof4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide(BMS-582949),aclinicalp38αMAPkinaseinhibitorforthetreatmentofinflammatorydiseases.JMedChem.2010Sep23McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forre