| Bioactivity | LY255283 is a LTB4 receptor (BLT2) antagonist, with an IC50 of ~100 nM for [3H]LTB4 binding to guinea pig lung membranes[1][2][3][4]. |
| Invitro | LY255283 competitively reduces conlractilc responses of lung parcnchyma to LTB, (pA2 = 7.2)[2].LY255283 (10 μM, 7 days) significantly suppresses the invasiveness of highly aggressive 253 J-BV bladder cancer cells[4]. Cell Viability Assay[4] Cell Line: |
| In Vivo | LY255283 (3, 30 mg/kg) ameliorates lipopolysaccharide-induced ARDS in pigs, possibly by blocking the recruitment of activated PMNs into alveoli in a dose-dependent fashion[3].LY255283 (2.5 mg/kg, ip) inhibits transitional cell carcinoma metastasis in mice models. The result suggests that a BLT2–Nox–ROS–NF–κB cascade plays a critical role in bladder cancer invasion and metastasis[4]. Animal Model: |
| Name | LY255283 |
| CAS | 117690-79-6 |
| Formula | C19H28N4O3 |
| Molar Mass | 360.45 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | -20°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen) |
| Reference | [1]. R M Schultz, et al. Effects of two leukotriene B4 (LTB4) receptor antagonists (LY255283 and SC-41930) on LTB4-induced human neutrophil adhesion and superoxide production. Prostaglandins Leukot Essent Fatty Acids. 1991 Aug;43(4):267-71. [2]. S A Silbaugh, et al. Pulmonary actions of LY255283, a leukotriene B4 receptor antagonist. Eur J Pharmacol. 1992 Nov 13;223(1):57-64. [3]. P S Wollert, et al. LY255283, a novel leukotriene B4 receptor antagonist, limits activation of neutrophils and prevents acute lung injury induced by endotoxin in pigs. Surgery. 1993 Aug;114(2):191-8. [4]. Eun-Young Kim, et al. BLT2 promotes the invasion and metastasis of aggressive bladder cancer cells through a reactive oxygen species-linked pathway. Free Radic Biol Med. 2010 Sep 15;49(6):1072-81. |