CP 105,696

CP 105,696 is an antagonist of the leukotriene B₄ (LTB₄) receptor (IC₅₀ = 8.42 nM for the high-affinity receptor in human neutrophils).¹ It inhibits chemotaxis induced by LTB₄ (Item No. 20110) in isolated human neutrophils (IC₅₀ = 5 nM) and LTB₄-induced calcium mobilization in isolated human monocytes (IC₅₀ = 940 nM). CP 105,696 reduces infiltration of neutrophils and eosinophils induced by arachidonic acid (Item Nos. 90010 | 90010.1 | 10006607) in guinea pig skin (ED₅₀ = 0.3 mg/kg, p.o.). It decreases blood glucose levels in the glucose tolerance test and reduces hepatic steatosis in a mouse model of obesity induced by a high-fat diet.² CP 105,696 decreases disease severity in a mouse model of experimental allergic encephalomyelitis (EAE; ED₅₀ = 8.6 mg/kg).³ It increases graft survival in a mouse model of allogeneic heart transplantation when administered at a dose of 50 mg/kg.⁴

WARNING This product is not for human or veterinary use.

1. Showell, H.J., Pettipher, E.R., Cheng, J.B., 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. 273(1), 176-184 (1995).

2. Li, P., Oh, D.Y., Bandyopadhyay, G., et al. LTB₄ promotes insulin resistance in obese mice by acting on macrophages, hepatocytes and myocytes. Nat. Med. 21(3), 239-247 (2015).

3. Gladue, R.P., Carroll, L.A., Milici, A.J., et al. Inhibition of leukotriene B₄-receptor interaction suppresses eosinophil infiltration and disease pathology in a murine model of experimental allergic encephalomyelitis. J. Exp. Med. 183(4), 1893-1898 (1996).

4. Weringer, E.J., Perry, B.D., Sawyer, P.S., et al. Antagonizing leukotriene B₄ receptors delays cardiac allograft rejection in mice. Transplantation 67(6), 808-815 (2024).