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Amelubant (BIIL 284) is a prodrug of active metabolites BIIL 260 and BIIL 315 with anti-inflammatory activity[1]. It is a potent, oral, long-acting LTB4 receptor antagonist that negligibly binds to the LTB4 receptor, exhibiting Kis of 221 nM and 230 nM in vital cells and membranes.
Description | Amelubant (BIIL 284) is a prodrug of active metabolites BIIL 260 and BIIL 315 with anti-inflammatory activity[1]. It is a potent, oral, long-acting LTB4 receptor antagonist that negligibly binds to the LTB4 receptor, exhibiting Kis of 221 nM and 230 nM in vital cells and membranes. |
Targets&IC50 | LTB4:221 nM (ki)( in vital human granulocytes), LTB4:230 nM (ki)( in cell membranes) |
In vitro | Amelubant is a prodrug of active metabolites BIIL 260 and BIIL 315, which are reversible and competitive LTB4 receptor antagonists with Kis of 1.4 and 1.1 nM in cells, and 1.7 and 1.9 nM in membranes, respectively [1]. |
Alias | BIIL 284 |
Molecular Weight | 538.63 |
Formula | C33H34N2O5 |
Cas No. | 346735-24-8 |
Relative Density. | 1.15 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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