Bimosiamose is a pan-selectin inhibitor (IC50s = 88, 20, and 86 ?M for E-, P-, and L-selectin, respectively).1 It reduces adhesion of HL-60 cells to E- and P-selectin when used at a concentration of 129 ?M.2 In vivo, bimosiamose (200 mg/kg) reduces skin scaliness, induration, and erythema in a patient-derived xenograft mouse model of psoriasis. It decreases hepatic alanine aminotransferase (ALT), aspartate aminotransferase (AST), lactate dehydrogenase (LDH), and myeloperoxidase (MPO) levels and reduces neutrophil infiltration in a rat model of severe hepatic ischemia-reperfusion injury.1 Bimosiamose also prevents nematode-induced late airway reactivity in sheep and reduces airway hyperresponsiveness in a mouse model of asthma.3
1.Palma-Vargas, J.M., Toledo-Pereyra, L., Dean, R.E., et al.Small-molecule selectin inhibitor protects against liver inflammatory response after ischemia and reperfusionJ. Am. Coll. Surg.185(4)365-372(1997) 2.Friedrich, M., Bock, D., Philipp, S., et al.Pan-selectin antagonism improves psoriasis manifestation in mice and manArch. Dermatol. Res.297(8)345-351(2008) 3.Aydt, E., and Wolff, G.Development of synthetic pan-selectin antagonists: A new treatment strategy for chronic inflammation in asthmaPathobiology70(5)297-301(2002)