Setipafant is a platelet-activating factor (PAF) antagonist.

PAF^[1]

Animals are separated into six groups: U₄, controls; S, sham operated animals undergoing laparotomy; I₄and I₉, ligation of the mesenteric vessels in the last ileal loop; IT₄and IT₉, same procedure together with treatment with Setipafant (50 mg/kg) orally before and after surgery and intraperitoneally during surgery. Animals are killed at day 4 in groups U₄, S, I₄and IT₄and at day 9 in groups I₉and IT₉, with histological studies and mediator measurements taken. Macroscopic and histological lesions of intestinal wall in groups I₄, I₉, IT₄and IT₉are similar to those of human neonatal necrotizing enterocolitis and do not vary according to the absence or the presence of Setipafant (BN 50727) treatment. Peritoneal bands are significantly reduced in treated groups IT₄and IT₉as compared with untreated ones I₄and I₉. Mucosal PAF levels in the terminal ileum are higher in group I₄than in groups U₄or I₉. In the upper loop, mucosal PAF levels are comparable in all groups. An increase in stool PAF levels is observed only in group I₉, whereas values comparable to those observed in controls are detected in other groups^[1]. Pretreatment of the animals with one or other of the structurally unrelated PAF receptor antagonists, BN 52021 (10 mg/kg, i.p.) or BN 50727 (1 mg/kg, i.p.) significantly reduces Dexamethasone-induced gastric damage. In these animals neither petechiae nor erosions are observed^[2].

519.02

C₂₆H₂₃ClN₆O₂S

132418-35-0

司替帕泛

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.