Bimosiamose (TBC-1269) is a nonoligosaccharide pan-selectin antagonist with IC 50 s of 88 μM, 20 μM, and 86 μM for E-selectin, P-selectin, and L-selectin, respectively. Bimosiamose has anti-inflammatory effects.
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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[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.
溶解度数据
In Vitro: DMSO : 100 mg/mL (115.89 mM; Need ultrasonic)0.1 M NaOH : 25 mg/mL (28.97 mM; ultrasonic and adjust pH to 10 with NaOH)配制储备液