(R)-Lisofylline

LSF, a chiral metabolite of pentoxifylline, acts as a potent anti-inflammatory agent.^1,2 (R)-LSF is the biologically active isomer of LSF.^1,2 It is a potent inhibitor of the generation of phosphatidic acid (IC₅₀ = 0.6 µM) from cytokine-activated lysophosphatidic acyl transferase (LPAAT), which has been shown to protect mice from endotoxic shock.³ (R)-LSF suppresses the production of the proinflammatory cytokine IFN-γ, inhibits interleukin 12-mediated STAT-4 activation, and enhances glucose-stimulated β-cell insulin secretion, reducing the onset of diabetes in a non-obese diabetic mouse model.^4,1

WARNING This product is not for human or veterinary use.

1. Yang, Z., Chen, M., Ellett, J.D., et al. Inflammatory blockade improves human pancreatic islet function and viability. Am. J. Transplant. 5(3), 475-483 (2005).

2. Wyska, E., Pekala, E., and Szymura-Oleksiak, J. Interconversion and tissue distribution of pentoxifylline and lisofylline in mice. Chirality 18(8), 644-651 (2006).

3. 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).

4. Yang, Z.D., Chen, M., Wu, R., et al. The anti-inflammatory compound lisofylline prevents type I diabetes in non-obese diabetic mice. Diabetologia 45(9), 1307-1314 (2002).