CP-105696 是一个有效的、白三烯 B₄ (LTB₄) 受体的选择性拮抗剂，其 IC₅₀ 值为 8.42 nM。

CP-105696 is a potent and selective Leukotriene B 4 Receptor antagonist, with an IC 50 of 8.42 nM.

Solid

LTB4 8.42±0.26 nM (IC50)

CP-105696 is a structurally novel, selective and potent LTB4 receptor antagonist. In vitro, CP-105696 inhibits [H]LTB4 (0.3 nM) binding to high-affinity LTB4 receptors on human neutrophils with an lC50 value of 8.42±0.26 nM. Scatchard analyses of [H]LTB4 binding to these high-affinity receptors indicate that CP-105696 acts as a noncompetitive antagonist. CP-105696 inhibits human neutrophil chemotaxis mediated by LTB4 (5 nM) in a noncompetitive manner with an IC50 value of 5.0±2.0 nM. Scatchard analyses of [H]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±0.19). CP-1056

At a dose of 50 mg/kg/day (28 days), B10.BR (H2k) allografts transplanted into C57Bl/6 (H2b) recipients are significantly protected, as reflected by the mean survival time versus control grafts (27±20 days [n=10] vs. 12±6 days [n=14]; P=0.0146). 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). Syngeneic grafts survive indefinitely (n=11). Immunohistological evaluation of allografts at rejection reveals a mononuclear cell infiltrate composed primarily of CD3+ and CD11b+ (Mac-1+) cells, which are infrequent in syngeneic grafts. 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, as demonstrated by CD11b staini

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Showell HJ, et al. The in vitro and in vivo pharmacologic activity of the potent and selective leukotriene B4 receptor antagonist CP-105696. J Pharmacol Exp Ther. 1995 Apr;273(1):176-84.
[2]. Weringer EJ, et al. Antagonizing leukotriene B4 receptors delays cardiac allograft rejection in mice. Transplantation. 1999 Mar 27;67(6):808-15.

In Vitro: DMSO : 100 mg/mL (233.36 mM; Need ultrasonic)配制储备液