CP-105696 is a selective antagonist of Leukotriene B4 Receptor (IC50: 8.42 nM).

CP-105696 inhibits human neutrophil chemotaxis mediated by LTB4 (5 nM) in a noncompetitive manner (IC50: 5.0 nM). CP-105696 inhibits [3H]LTB4 (0.3 nM) binding to high-affinity LTB4 receptors on human neutrophils (lC50: 8.42 nM). Scatchard analyses of [3H]LTB4 binding to low-affinity receptors on neutrophils indicate that CP-105696 acts as a competitive antagonist at this receptor, and inhibition of LTB4-mediated CD11b upregulation on human neutrophils is competitively inhibited by CP-105696 (pA2=8.03). CP-105696 (10 μM) treatment does not inhibit either human neutrophil chemotaxis or CD11b upregulation mediated through alternate (i.e., C5a, lL-8, PAF) G-protein coupled chemotactic factor receptors. In isolated human monocytes, LTB4 (5 nM)-mediated Ca2+ mobilization is inhibited by CP-105696 (lC50: 940 nM) [1].

Using an induction protocol (day -1 to day 3), CP-105696 at 100 mg/kg/day significantly prolongs allograft survival (33±23 days [n=9]; P=0.0026), but CP-105696 at 10 mg/kg/day does not (18±16 days [n=8]; P=0.1433). Allografts from mice treated with CP-105696 at 50 or 100 mg/kg/day demonstrat a selective reduction in β2-integrin (Mac-1) expression on monocytes/macrophages [2].

158081-99-3

C28H28O4

428.52

Pfizer 105696

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years