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经验公式(希尔记法):
C19H28N4O3
化学文摘社编号:
分子量:
360.45
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352204
MDL number:
产品名称
LY255283, ≥98% (HPLC), powder
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)
SMILES string
CCc1cc(C(C)=O)c(O)cc1OCCCCCC(C)(C)c2nnn[nH]2
InChI key
WCGXJPFHTHQNJL-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
powder
color
off-white to light yellow
solubility
DMSO: >20 mg/mL
originator
Eli Lilly
storage temp.
−20°C
Quality Level
Application
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.
Biochem/physiol Actions
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.
Features and Benefits
This compound was developed by Eli Lilly. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.
存储类别
11 - Combustible Solids
wgk
WGK 2
flash_point_f
Not applicable
flash_point_c
Not applicable
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
Eun-Young Kim et al.
Free radical biology & medicine, 49(6), 1072-1081 (2010-07-06)
Aggressive bladder cancer is a major cause of morbidity and mortality. Despite the fact that metastatic disease results in death in the majority of bladder cancer cases, the molecular events regulating the invasive phenotype of aggressive bladder cancer are not
J S Sawyer et al.
Journal of medicinal chemistry, 38(22), 4411-4432 (1995-10-27)
Structural derivatives of LY255283 have been studied as receptor antagonists of leukotriene B4. Substitution of the 2-hydroxyacetophenone subunit of 1 (LY255283) with a 2-arylphenol group provided entry into several new series that feature various mono- and diacidic core functionality. These
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
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
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