Etalocib (LY293111) produces a dose-related inhibition of acute leukotriene B 4 -induced airway obstruction when administered i.v. (ED 50 =14 µg/kg) or p.o. (ED 50 =0.4 mg/kg). Etalocib (LY293111, 10 mg/kg) inhibits A23187-induced lung inflammatory changes at 1 h. Etalocib (LY293111, 250 mg/kg/day, orally) inhibits growth of human pancreatic cancer xenografts in athymic mice. Animal Model: Guinea pigs. Dosage: 1-10 mg/kg. Administration: Orally once. Result: A single 1 mg/kg oral dose inhibited excised lung gas volume increases by 76.7±7.1% (n=4, P<0.002) when given 8 h prior to leukotriene B 4 challenge, and 28.6±20.3% (n=4, NS) when given 24 h before challenge. Had no effect (10 mg/kg) on pulmonary gas trapping at 1 h or 2 h after A23187 challenge. However, at 4 h, the pulmonary gas trapping response was significantly less than that of vehicle-treated controls and not different from sham values. The 10 mg/kg dose inhibited A23187-induced lung inflammatory changes at 1 h, but was without effect at 2 h or 4 h after challenge.

Etalocib (LY293111) elicits a concentration-dependent inhibition of LTB 4 induced CD11b up-regulation. Etalocib (LY293111) is an extremely potent and selective antagonist of human neutrophil function in vitro. Etalocib (LY293111, 250 and 500 nM, 24-72 h) induces apoptosis and inhibits proliferation in human pancreatic cancer cells. Cell Proliferation Assay Cell Line: MiaPaCa-2 and AsPC-1 human pancreatic cancer cells. [3] Concentration: 500 nM. Incubation Time: 24, 48, and 72 h. Result: Caused both a concentration-dependent and time-dependent inhibition of thymidine incorporation in both MiaPaCa-2 and AsPC-1 human pancreatic cancer cells. Apoptosis Analysis Cell Line: MiaPaCa-2 and AsPC-1 human pancreatic cancer cells. Concentration: 250 and 500 nM. Incubation Time: 24 h. Result: Induced apoptosis in human pancreatic cancer cells.

Etalocib (LY293111) 是具有口服活性的白三烯 (LTB4) 受体的拮抗剂，抑制 [3H]LTB4 结合的Ki 值为 25 nM. Etalocib (LY293111) 抑制LTB4 诱导的钙动员的 lC50 值为 20 nM。Etalocib (LY293111) 可诱导凋亡。