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

更新时间：2024-01-09 18:50:58

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-酮结构式	常用名	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	英文名	LY255283
	CAS号	117690-79-6	分子量	360.451
	密度	1.2±0.1 g/cm3	沸点	573.4±60.0 °C at 760 mmHg
	分子式	C₁₉H₂₈N₄O₃	熔点	160-162 °C
	MSDS	美版	闪点	300.6±32.9 °C

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。

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	1-[5-ethyl-2-hydroxy-4-[6-methyl-6-(2H-tetrazol-5-yl)heptoxy]phenyl]ethanone
英文别名	更多

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.

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

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%

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1-(5-Ethyl-2-hydroxy-4-(6-methyl-6-(1H-tetrazol-5-yl)heptyloxy)phenyl)ethanone

1-(5-Ethyl-2-hydroxy-4-{[6-methyl-6-(2H-tetrazol-5-yl)heptyl]oxy}phenyl)ethanone

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