6-(4-FLUOROPHENYL)-2,3-DIHYDRO-5-(4-PYRIDINYL)IMIDAZO[2,1-B]THIAZOLE DIHYDROCHLORIDE

Description

SKF 86002 is an anti-inflammatory agent. It inhibits rat seminal vesicle prostaglandin H₂ (PGH₂) synthase (IC₅₀ = 120 μM), as well as prostanoid production by rat basophilic leukemia (RBL-1) cells and human monocytes (IC₅₀s = 70 and 1 μM, respectively). SKF 86002 inhibits leukotriene B₄ (LTB₄) and LTC₄ production induced by A23187 in human neutrophils and monocytes, respectively (IC₅₀ = 20 μM for both). It also inhibits LPS-induced IL-1 production in human monocytes (IC₅₀ = 1.3 μM). SKF 86002 (10, 30, and 90 mg/kg) reduces hindleg volume in rat models of adjuvant- or collagen-induced arthritis. It also decreases serum levels of TNF-α and increases survival in a mouse model of LPS and galactosamine-induced endotoxic shock when administered at a dose of 100 mg/kg.

Uses

SKF 86002 is an inhibitor of p53, Cox, and 5-LO.

Definition

ChEBI: 6-(4-fluorophenyl)-5-pyridin-4-yl-2,3-dihydroimidazo[2,1-b]thiazole is a member of imidazoles.

Biological Activity

Inhibitor of p38 MAP kinase (IC 50 = 0.1-1 μ M). Potently inhibits LPS-induced IL-1 and TNF- α production in human monocytes (IC 50 = 1 μ M). Also inhibits 5-lipoxygenase- and cyclooxygenase-mediated arachidonic acid metabolism in RBL-1 cells (IC 50 values are 10 and 100 μ M respectively). Anti-inflammatory following oral administration in vivo .