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质量水平
方案
≥98% (HPLC)
表单
powder
颜色
off-white to light yellow
溶解性
DMSO: >20 mg/mL
创始人
Eli Lilly
储存温度
−20°C
SMILES字符串
CCc1cc(C(C)=O)c(O)cc1OCCCCCC(C)(C)c2nnn[nH]2
InChI
1S/C19H28N4O3/c1-5-14-11-15(13(2)24)16(25)12-17(14)26-10-8-6-7-9-19(3,4)18-20-22-23-21-18/h11-12,25H,5-10H2,1-4H3,(H,20,21,22,23)
InChI key
WCGXJPFHTHQNJL-UHFFFAOYSA-N
应用
LY255283, a competitive leukotriene B4 receptor antagonist, is used in leukotriene receptor research along with other selective leukotriene receptor agonists and antagonist to identify and differentiate the physiological and cell signaling effects of the leukotriene B4 receptor on processes such as paclitaxel resistance in MCF-7/DOX breast cancer cells, monocyte-derived dendritic cell chemotaxis, and 5-lipoxygenase activity and interleukin-8 production in human neutrophils. LY255283 may be used to help verify that an observed process or cell event is leukotriene B4 receptor-dependent.
生化/生理作用
LY255283 is a competitive leukotriene B4 receptor antagonist, specific to the BLT2 receptor subtype.
LY255283 is a competitive leukotriene B4 receptor antagonist, with an IC50 of about 100 nM. It is somewhat selective for the BLT2 receptor, since IC50 values at the BLT1 receptor are >10 μM. LY255283 reduces airway obstruction in animal models of asthma.
特点和优势
This compound was developed by Eli Lilly. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.
储存分类代码
11 - Combustible Solids
WGK
WGK 2
闪点(°F)
Not applicable
闪点(°C)
Not applicable
P S Wollert et al.
Surgery, 114(2), 191-198 (1993-08-01)
Polymorphonuclear neutrophils (PMNs) have been implicated in the pathogenesis of the adult respiratory distress syndrome (ARDS). Because leukotriene B4 (LTB4) is a potent activator of PMNs, we sought to determine whether LY255283, an LTB4 receptor antagonist, could block PMN activation
J Wijkander et al.
The Journal of biological chemistry, 270(44), 26543-26549 (1995-11-03)
Addition of submicromolar concentrations of arachidonic acid (AA) to human neutrophils induced a 2-fold increase in the activity of a cytosolic phospholipase A2 (PLA2) when measured using sonicated vesicles of 1-stearoyl-2-[14C]arachidonoylphosphatidylcholine as substrate. A similar increase in cytosolic PLA2 activity
Anne-Sofie Johansson et al.
Prostaglandins, leukotrienes, and essential fatty acids, 84(3-4), 109-112 (2010-12-25)
Leukotriene B4 (LTB4), a potent chemotactic and immune-modulating lipid mediator, signals via two receptors, BLT1 and BLT2, leading to pro-inflammatory responses in phagocytes. Recently, we reported that BLT1 is the predominating BLT on human umbilical vein endothelial cells (HUVEC) and
Jin-Wook Lee et al.
The Journal of biological chemistry, 288(42), 30054-30063 (2013-08-30)
The majority of prostate cancer-related deaths are associated with advanced and metastatic malignancies. Although anoikis resistance has been recognized as one of the hallmarks of metastatic prostate malignancies, the molecular events that cause anoikis resistance are poorly understood. In this
M P Fink et al.
Critical care medicine, 21(12), 1825-1837 (1993-12-01)
To evaluate the hypothesis that treatment with LY255283, a novel leukotriene B4-receptor antagonist, is beneficial in an animal model of the adult respiratory distress syndrome induced by endotoxin. Prospective, randomized, controlled trial. Laboratory at a large university medical center. Twenty-five
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