ZM 230487

ZM 230487 is an orally active, selective, non-redox 5-lipoxygenase (5-LO) inhibitor. ZM 230487 potently inhibits antigen-induced LTD₄ release (IC₅₀ ≈ 0.2 µM), but does not affect the release of TXB₂ and histamine. ZM 230487 specifically blocks eosinophil accumulation and partial bronchoconstriction in guinea pig models. ZM 230487 can be used in studies related to allergic inflammation^[1][2]. In Vitro:ZM 230487 (0.03-1.0 μM) potently inhibits antigen-induced leukotriene D₄ release from sensitized guinea pig lung parenchymal fragments prepared in vitro, with an IC₅₀ of 0.2 μM, but exerts no significant effect on antigen-induced thromboxane B₂ or histamine release^[2]. In Vivo:ZM 230487 (1 pmol-100 nmol per site; intradermal injection; single administration) potently inhibits arachidonic acid (AA) (HY-109590)-induced eosinophil accumulation in guinea pig skin, with an IC₅₀ of approximately 2 pmol per site, but only partially inhibits the associated mild edema formation^[1].
ZM 230487 (10 nmol per site; intradermal injection; single administration) significantly inhibits eosinophil accumulation (with an inhibition rate of 44%-72%), but exerts no effect on edema formation in the guinea pig passive cutaneous anaphylaxis model^[1].
ZM 230487 (1 mg/kg; intravenous injection; single administration) potently inhibits antigen-induced bronchoconstriction in passively sensitized guinea pigs with an inhibition rate of 90%, and exerts no non-specific effect on methacholine-induced pulmonary responses^[2].
ZM 230487 (0.4 mg/kg; p.o.; single administration) potently inhibits leukotriene B₄ synthesis in a zymosan-induced inflammatory rat air pouch model, with an oral ED₅₀ of 0.4 mg/kg at 3 h post-administration^[2].