Leukotriene B4 (LTB4) is a dihydroxy fatty acid derived from the 5-lipoxygenase pathway of arachidonic acid metabolism and is an important mediator of the inflammatory process. LY293111 is a potent antagonist of the LTB4 receptor, BLT1, that inhibits the specific binding of radiolabeled-LTB4 to isolated human neutrophils with an IC50 value of 17.6 nM and inhibits the LTB4-induced chemotaxis of human neutrophils with an IC50 value of 6.3 nM.1 LY293111 inhibits growth of MiaPaCa-2 and AsPC-1 human pancreatic cancer cells in vitro (250-1,000 nM) and subcutaneous xenografts in athymic mice (250 mg/kg/day), inducing apoptosis and S-phase arrest.2
1
Jackson, W.T., Froelich, L.L., Boyd, R.J., et al. Pharmacologic actions of the second-generation leukotriene B4 receptor antagonist LY293111: In vitro studies. J Pharmacol Exp Ther288(1)286-294(1999).
2
Tong, W., Ding, X., Hennig, R., et al. Leukotriene B4 receptor antagonist LY293111 inhibits proliferation and induces apoptosis in human pancreatic cancer cells. Clin Cancer Res83232-3242(2002).
Jackson, W.T., Froelich, L.L., Boyd, R.J., et al. Pharmacologic actions of the second-generation leukotriene B4 receptor antagonist LY293111: In vitro studies. J Pharmacol Exp Ther288(1)286-294(1999).
Tong, W., Ding, X., Hennig, R., et al. Leukotriene B4 receptor antagonist LY293111 inhibits proliferation and induces apoptosis in human pancreatic cancer cells. Clin Cancer Res83232-3242(2002).
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