| Bioactivity | 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]. | ||||||||||||
| Target | IC50: 88 μM (E-selectin), 20 μM (P-selectin), 86 μM (L-selectin) | ||||||||||||
| Invitro | 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]. Animal Model: | ||||||||||||
| Name | Bimosiamose | ||||||||||||
| CAS | 187269-40-5 | ||||||||||||
| Formula | C46H54O16 | ||||||||||||
| Molar Mass | 862.91 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Palma-Vargas JM, et al. Small-molecule selectin inhibitor protects against liver inflammatory response after ischemia and reperfusion. J Am Coll Surg. 1997 Oct;185(4):365-72. |