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1-(5-乙基-2-羟基-4-((6-甲基-6-(2H-四唑-5-基)庚基)氧基)苯基)乙-1-酮

用途

LY255283 是 LTB4 受体 (BLT2) 的拮抗剂,其抑制 [3H]LTB4 结合到豚鼠肺膜的 IC50 值约为 100 nM。

名称

[ CAS 号 ]:
117690-79-6

[ 中文名 ]:
1-[5-乙基-2-羟基-4-[[6-甲基-6-(1H-四唑-5-基)庚基]氧基]苯基]乙酮

[ 英文名 ]:
LY255283

[英文别名 ]:

生物活性

[ 描述 ]:

LY255283 是 LTB4 受体 (BLT2) 的拮抗剂,其抑制 [3H]LTB4 结合到豚鼠肺膜的 IC50 值约为 100 nM。

[ 相关类别 ]:

研究领域 >> 癌症

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 白三烯受体

研究领域 >> 炎症/免疫

[ 靶点 ]

LTB4:~100 nM (IC50, LTB4 binds to guinea pig lung membranes)

[体外研究]

LY255283完全降低肺实质对LTB的反应,(pA2=7.2)[2]。LY255283(10μM,7天)可显著抑制253例J-BV膀胱癌细胞的侵袭性[4]。细胞活力测定[4]细胞系：253个J-BV细胞。浓度：5或10μM,培养时间：7天。结果：抑制BLT2信号可减弱253株J-BV细胞的侵袭性迁移。

[体内研究]

LY255283(3,30mg/kg)可能通过以剂量依赖性的方式阻断激活的PMNs进入肺泡的募集,改善了脂多糖诱导的ARDS。LY255283(2.5mg/kg,ip)抑制小鼠移行细胞癌转移。结果表明,BLT2–Nox–ROS–NF–κB级联在膀胱癌的侵袭和转移中起关键作用[4]。动物模型：小鼠(注射253个J-BV细胞)[4]。剂量：2.5mg/kg。给药：注射细胞后3天和5天注射IP。结果：注射后12周,小鼠经LY255283处理后,每个肺仅形成0～3个结节,组织学分析证实微转移灶数量明显减少。

[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.

物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
573.4±60.0 °C at 760 mmHg

[ 熔点 ]:
160-162 °C

[ 分子式 ]:
C₁₉H₂₈N₄O₃

[ 分子量 ]:
360.451

[ 闪点 ]:
300.6±32.9 °C

[ 精确质量 ]:
360.216156

[ PSA ]:
100.99000

[ LogP ]:
4.04

[ 外观性状 ]:
固体

[ 蒸汽压 ]:
0.0±1.6 mmHg at 25°C

[ 折射率 ]:
1.553

[ 储存条件 ]:
-20°C，惰性气体

安全信息

[ 危害码 (欧洲) ]:
F+

[ 危险品运输编码 ]:
NONH for all modes of transport

[ 海关编码 ]:
2933990090

海关

[ 海关编码 ]: 2933990090

[ 中文概述 ]:
2933990090. 其他仅含氮杂原子的杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

文献

Leukotriene B4 Inhibits L-Type Calcium Channels via p38 Signaling Pathway in Vascular Smooth Muscle Cells.

Cell Physiol. Biochem. 37 , 1903-13, (2015)

Arachidonic acid (AA) and its metabolites are important endogenous lipid messengers. In this study, we test the effect of Leukotriene B4 (LTB4), a 5-lipoxygenase metabolite of AA, on L-type calcium ch...

12-Hydroxyheptadecatrienoic acid promotes epidermal wound healing by accelerating keratinocyte migration via the BLT2 receptor.

J. Exp. Med. 211(6) , 1063-78, (2014)

Leukotriene B4 (LTB4) receptor type 2 (BLT2) is a G protein-coupled receptor (GPCR) for 12(S)-hydroxyheptadeca-5Z,8E,10E-trienoic acid (12-HHT) and LTB4. Despite the well-defined proinflammatory roles...

A leukotriene B4 receptor-2 is associated with paclitaxel resistance in MCF-7/DOX breast cancer cells.

Br. J. Cancer 109(2) , 351-9, (2013)

Breast cancer is the most common malignancy in women. Although chemotherapeutic agents, such as paclitaxel, are effective treatments for the majority of breast cancer patients, recurrence is frequent ...

更多文献

1-(5-乙基-2-羟基-4-((6-甲基-6-(2H-四唑-5-基)庚基)氧基)苯基)乙-1-酮

用途

名称

生物活性

物理化学性质

安全信息

海关

文献

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