T-5224T-5224 is a selective inhibitor of c-Fos/activator protein (AP)-1, attenuates lipopolysaccharide-induced liver injury in mice.
IC50 value:
Target: c-Fos/AP1 inhibitor
in vitro: T-5224 was converted to its acyl O-glucuronide (G2) by UGT1A1 and UGT1A3 and to its hydroxyl O-glucuronide (G3) by several UGTs, but it was not metabolized by the P450s [2].
in vivo: Administration of T-5224 (300 mg kg(-1), p.o.) after intraperitoneal injection of LPS imparted appreciable protection against acute elevations in serum levels of TNFα, HMGB1, ALT/AST as well as in liver tissue levels of MIP-1α and MCP-1, and reduced the lethality (27 %) [1].
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