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Catalog: | HY-106139 |
Brand: | MCE |
CAS: | 187269-40-5 |
MDL | - |
---|---|
Molecular Weight | 862.91 |
Molecular Formula | C46H54O16 |
SMILES | OC[C@H]([C@@H](O)[C@H](O)[C@@H]1O)O[C@@H]1OC(C=C2)=C(C3=CC(CC(O)=O)=CC=C3)C=C2CCCCCCC(C=C4)=CC(C5=CC(CC(O)=O)=CC=C5)=C4O[C@H]6O[C@@H]([C@@H](O)[C@H](O)[C@@H]6O)CO |
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 [1] .
IC50: 88 μM (E-selectin), 20 μM (P-selectin), 86 μM (L-selectin) [1]
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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: | Sprague-Dawley rats (200-225g) with ischemia and reperfusion (I/R) [1] |
Dosage: | 25 mg/kg |
Administration: | Intravenous injection |
Result: | Showed a significant increase in survival compared with controls. |
NCT Number | Sponsor | Condition | Start Date | Phase |
---|---|---|---|---|
NCT00823693 | Revotar Biopharmaceuticals AG |
Psoriasis
|
Phase 2 | |
NCT00962481 | Revotar Biopharmaceuticals AG |
Chronic Obstructive Pulmonary Disease (COPD)
|
Phase 2 | |
NCT01108913 | Revotar Biopharmaceuticals AG |
Chronic Obstructive Pulmonary Disease
|
Phase 2 |
Solid
Room temperature in continental US; may vary elsewhere.
Powder | -20°C | 3 years |
---|---|---|
4°C | 2 years | |
In solvent | -80°C | 6 months |
-20°C | 1 month |
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)
Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
---|
1 mM | 1.1589 mL | 5.7943 mL | 11.5887 mL |
5 mM | 0.2318 mL | 1.1589 mL | 2.3177 mL |
10 mM | 0.1159 mL | 0.5794 mL | 1.1589 mL |
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