| 产品描述: | LY255283 is a LTB4 receptor (BLT2) antagonist, with an IC50 of ~100 nM for [3H]LTB4 binding to guinea pig lung membranes |
| 靶点: |
LTB4:~100 nM (IC50, LTB4 binds to guinea pig lung membranes);LeukotrieneReceptor |
| 体外研究: |
LY255283 竞争性降低肺实质对 LTB 的收缩反应,(pA2=7.2)。 LY255283 (10 μM,7 天) 显著抑制高侵袭性 253 J-BV 膀胱癌细胞的侵袭性。 Cell Viability Assay Cell Line: 253 J-BV cells. Concentration: 5 or 10 μM. Incubation Time: 7 days. Result: Inhibition of BLT2 signaling attenuates aggressive migration by 253 J-BV cells. |
| 体内研究: |
LY255283 (3,30 mg/kg) 可改善猪体内脂多糖诱导的 ARDS,这可能是通过以剂量依赖性方式阻断活化的 PMN 募集到肺泡中。 LY255283 (2.5 mg/kg,ip) 在小鼠模型中抑制移行细胞癌转移。结果表明,BLT2-Nox-ROS-NF-κB级联在膀胱癌侵袭和转移中起关键作用。 Animal Model: Mice (253 J-BV cells injected). Dosage: 2.5 mg/kg. Administration: IP injected 3 and 5 days after injection of cells. Result: By 12 weeks after injection, in mice treated with LY255283 only 0-3 nodules formed per lung, and histological analysis confirmed that the number of micrometastatic lesions was markedly reduced. |
| 参考文献: |
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. |
| 溶解性: |
Soluble in DMSO |
| 保存条件: |
-20℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.774 ml |
13.872 ml |
27.743 ml |
| 5 mM |
0.555 ml |
2.774 ml |
5.549 ml |
| 10 mM |
0.277 ml |
1.387 ml |
2.774 ml |
| 50 mM |
0.055 ml |
0.277 ml |
0.555 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |