Bimosiamose

Bimosiamose (TBC-1269) is a nonoligosaccharide pan-selectin antagonist with IC₅₀s of 88 μM, 20 μM, and 86 μM for E-selectin, P-selectin, and L-selectin, respectively. Bimosiamose has anti-inflammatory effects^[1]. IC50 & Target:IC50: 88 μM (E-selectin), 20 μM (P-selectin), 86 μM (L-selectin)^[1] In Vitro:Bimosiamose (TBC-1269) operates by inhibiting neutrophil recruitment to the site of inflammation through blocking the initial rolling phase of recruitment. Bimosiamose (TBC-1269) inhibits cell recruitment and does not possess any cytotoxic effect on neutrophils^[1]. In Vivo:Bimosiamose (TBC-1269; 25 mg/kg; intravenous injection; Sprague-Dawley rats) treatment shows a significant increase in survival. Best overall survival, 70%, is observed when TBC-1269 is administered 15 minutes before reperfusion, and also shows a marked decrease in liver enzyme levels at 6 hours after reperfusion. Neutrophil migration is also significantly ameliorated (81%). The histologic damage scores is also improved^[1].