TofacitinibisaninhibitorofJAK1/2/3thatisclinicallyusedtotreatmyelofibrosisandrheumatoidarthritis.Tofacitinibexhibitsimmunosuppressive,anti-inflammatory,andantiviralactivities.Invitro,tofacitinibinhibitsproductionofinflammatorycytokines,Th4celldifferentiation,Th17celldifferentiation,andactivationofSTAT1,whichinturnpreventsinductionofT-betandgenerationofTh1cells.Inothercellularmodels,tofacitinibinhibitsHIVreplicationandreactivationoflatentHIV-1.
| CasNo. | 540737-29-9 |
|---|---|
| Purity | ≥99% |
| Formula | C16H20N6O•C6H8O7 |
| FormulaWt. | 504.49 |
| ChemicalName | 3-[(3R,4R)-4-methyl-3-[methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl]-3-oxopropanenitrilecitratesalt |
| IUPACName | 2-hydroxypropane-1,2,3-tricarboxylicacid;3-[(3R,4R)-4-methyl-3-[methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl]-3-oxopropanenitrile |
| Synonym | CP-690550-10,Tasocitinibcitratesalt |
| Appearance | Whitetooffwhitepowder |
| StoreTemp | Ambient |
|---|---|
| ShipTemp | Ambient |
| InfoSheet | T5720InfoSheetPDF |
|---|
GavegnanoC,DetorioM,MonteroC,etal.RuxolitinibandTofacitinibarePotentandSelectiveInhibitorsofHIV-1ReplicationandVirusReactivationinVitro.AntimicrobAgentsChemother.2014Jan13.[Epubaheadofprint].PMID:24419350.
YamaokaK,TanakaY.TargetingtheJanuskinasesinrheumatoidarthritis:focusontofacitinib.ExpertOpinPharmacother.2014Jan;15(1):103-13.PMID:4188100.
TakPP,KaldenJR.Advancesinrheumatology:newtargetedtherapeutics.ArthritisResTher.2011May25;13Suppl1:S5.PMID:21624184.
GhoreschiK,JessonMI,LiX,etal.Modulationofinnateandadaptiveimmuneresponsesbytofacitinib(CP-690,550).JImmunol.2011Apr1;186(7):4234-43.PMID:21383241.
