AS1940477 is p38 MAPK inhibitor. AS1940477 inhibited the enzymatic activity of recombinant p38alpha and beta isoforms but showed no effect against other 100 protein kinases including p38gamma and delta isoforms. In human peripheral blood mononuclear cells, AS1940477 inhibited lipopolysaccharide (LPS)- or phytohemagglutinin A (PHA)-induced production of proinflammatory cytokines, including TNFalpha, IL-1beta, and IL-6 at low concentrations (LPS/TNFalpha, IC(50)=0.45n M, PHA/TNFalpha, IC(50)=0.40 nM). In addition, equivalent concentrations of AS1940477 that inhibited cytokine production also inhibited TNFalpha- and IL-1 beta-induced production of IL-6, PGE(2), and MMP-3 in human synovial stromal cells. AS1940477 was also found to potently inhibit TNF production in whole blood (IC(50)=12 nM) and effectively inhibited TNFalpha production induced by systemically administered LPS in rats at less than 0.1mg/kg (ED(50)=0.053 mg/kg) with an anti-inflammatory effect lasting for 20h after oral administration. Overall, this stu......
Molekulargewicht:
431.46
CAS Nummer:
[928344-12-1]
Formel:
C24H22FN5O2
Target-Kategorie:
Others
T68321
* Mehrwertsteuer und Versandkosten nicht enthalten. Irrtümer und Preisänderungen vorbehalten
