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CP-105,696 is an orally active, potent and selective leukotriene B4 receptor (LTB4R) antagonist (IC50 against [3H]LTB4 = 5.6 nM for binding human neutrophils; IC50 = 9.7 nM & 30.3 nM, respectively using guinea pig spleen or mouse membranes) that targets LTB4R high- and low-affinity binding sites in a LTB4 non-competitive and competitive manner, respectively. CP-105,696 inhibits 5 nM LTB4-induced human neutrophils chemotaxis and CDllb upregualtion (IC50 = 5.2 nM and 430 nM, respectively) without inhibiting cyclooxygenase activity or affecting chemotaxis induced by C5a, PAF, IL-8. Oral administration is efficacious against intradermal LTB4 (100 ng/mouse), but not IL-1, injection-induced neutrophil accumulation in mice and guinea pigs (ED50 = 4.2 and 0.26 mgkg, respectively). CP-105,696 in vivo efficacy is also demonstrated in other animal models, including collagen-induced arthritis (CIA; 0.3-10 mg/kg in mice), allergic encephalomyelitis (ED50= 8.6 mg/kg; mice), and asthma (10-30 mg/kg; primate).
| Molecular Weight | 428.52 |
| Formula | C28H28O4 |
| CAS Number | 158081-99-3 |
| Form | Solid |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Leukotriene Receptor Products |
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| Ablukast
Ablukast (Ro 23-3544) is a specific and active leukotriene receptor antagonist. |
| BIIL-260
BIIL-260 is a potent and long-acting orally active leukotriene B(4) receptor LTB4 antagonist, with anti-inflammatory activity. |
| Olsalazine
Olsalazine is a potent inhibitor of macrophages chemotaxis to LTB4 with an IC50 value of 0.39 mM. |
| HAMI 3379
HAMI 3379 is a potent and selective CysLT2 receptor antagonist. |
| FPL-55712 free base
FPL-55712 free base is a leukotriene receptor antagonist. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
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