Pentoxifylline

Pentoxifylline is a methylxanthine derivative. It has been shown to have anti-inflammatory activity, inhibiting LPS-induced TNF-α production in isolated peripheral blood mononuclear cells (IC₅₀ = 85 µM) and suppressing LPS-induced leukopenia in mice.¹ Pentoxifylline weakly inhibits the generation of phosphatidic acid (IC₅₀ = 500 µM) from LPS-activated lysophosphatidic acyl transferase (LPAAT), and weakly antagonizes A₁ and A₂ adenosine receptors.^2,3 It also inhibits human acidic mammalian chitinase, human chitotriosidase, and chitinase B1 from Aspergillus fumigatus (IC₅₀s = 49, 98, and 126 µM, respectively).⁴

WARNING This product is not for human or veterinary use.

1. Cottam, H.B., Shih, H., Tehrani, L.R., et al. Substituted xanthines, pteridinediones, and related compounds as potential antiinflammatory agents. Synthesis and biological evaluation of inhibitors of tumor necrosis factor α. J. Med. Chem. 39, 2-9 (1996).

2. Rice, G.C., Brown, P.A., Nelson, R.J., et al. Protection from endotoxic shock in mice by pharmacologic inhibition of phosphatidic acid. Proc. Natl. Acad. Sci. USA 91(9), 3857-3861 (1994).

3. Schwabe, U., Ukena, D., and Lohse, M.J. Xanthine derivatives as antagonists at A₁ and A₂ adenosine receptors. Naunyn Schmiedebergs Arch. Pharmacol. 330(3), 212-221 (1985).

4. Rao, F.V., Andersen, O.A., Vora, K.A., et al. Methylxanthine drugs are chitinase inhibitors: Investigation of inhibition and binding modes. Chem. Biol. 12(9), 973-980 (2005).