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ProductDescription
VX-702isanorally-available,aminopyridine-based,ATP-competitiveinhibitorofp38MAPKwithaKdof3.7nMand17nMat10uMforp38aandp38b,respectively.[1]InanexvivobloodassayprimedwithLPS<VX-702dose-dependentlyinhibitedtheproductionofIL-6,IL-1b,TNFaatIC50of59,122,and99ng/mL,respectively.[2]VX-702wasfoundtobeequivalenttoprednisoloneandmethotrexateinamousecollagen-inducedarthritismodel.
ClinicalefficacymodelsplustransientsuppressionofinflammationbioMarkerssuggestthatp38MAPKinhibitionbyagentssuchasVX-702maynotbeaviableapproachtothetreatmentofchronicinflammationinRA.[3]
Technicalinformation:
ChemicalFormula: | C19H12F4N4O2 | |
CAS#: | 479543-46-9 | |
MolecularWeight: | 404.32 | |
Purity: | >98% | |
Appearance: | White | |
ChemicalName: | 1-(5-carbamoyl-6-(2,4-difluorophenyl)pyridin-2-yl)-1-(2,6-difluorophenyl)urea | |
Solubility: | Upto100mMinDMSO | |
Synonyms: | VX-702,VX702 |
ShippingCondition:Theproductisshippedinaglassvialatambienttemperature.
Storagecondition:Forlongershelflife,storesolidpowderat4oCdesiccated,orstoreDMSOsolutionat-20oC.
Reference:
1. | Goldsteinetal.,Selectivep38alphainhibitorsclinicallyevaluatedforthetreatmentofchronicinflammatorydisorders.J.Med.Chem.2010,53,2345-2353.PubmedID:19950901 |
2. | Ding,C.,Drugevaluation:VX-702,aMAPkinaseinhibitorforrheumatoidarthritisandacutecoronarysyndrome.Curr.Opin.Invest.Drugs,2006,7(11),1020-1025.PubmedID:17117592 |
3. | Damjanovetal.,Efficacy,pharmacodynamics,andsafetyofVX-702,anovelp38MAPKinhibitor,inrheumatoidarthritis:resultsoftworandomized,double-blind,placebo-controlledclinicalstudies.ArthritisRheum.,2009,60(5),1232-1241.PubmedID:19404957 |
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