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4-(4-octadecylphenyl)-4-oxobut-2-enoic acid

用途

OBAA是一种有效的磷脂酶A2(PLA2)抑制剂,IC50为70 nM。OBAA阻断蜂毒素诱导的布氏锥虫Ca2+内流,IC50为0.4μM[1][2][3]。

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名称

[ CAS 号 ]:
134531-42-3

[ 中文名 ]:
3-(4-十八烷基)-苯甲酰丙烯酸

[ 英文名 ]:
OBAA

[英文别名 ]:

OBAA

生物活性

[ 描述 ]:

OBAA是一种有效的磷脂酶A2(PLA2)抑制剂,IC50为70 nM。OBAA阻断蜂毒素诱导的布氏锥虫Ca2+内流,IC50为0.4μM[1][2][3]。

[ 相关类别 ]:

信号通路 >> 细胞凋亡 >> 细胞凋亡

信号通路 >> 代谢酶/蛋白酶 >> 磷脂

研究领域 >> 炎症/免疫

[ 靶点 ]

PLA2:70 nM (IC50)

[体外研究]

OBAA(5.7μM)诱导人脐静脉内皮细胞(HUVEC)凋亡。治疗16小时后,几乎所有细胞都分裂成凋亡小体[1]。

[体内研究]

OBAA(2.5-7 mg/kg静脉注射)显著且剂量依赖性地抑制豚鼠免疫诱导的支气管痉挛[3]。

[参考文献]

[1]. J Y Miao, et al. Inhibitors of phospholipase promote apoptosis of human endothelial cells. J Biochem. 1997 Mar;121(3):612-8.

[2]. J Eintracht, et al. Calcium entry in Trypanosoma brucei is regulated by phospholipase A2 and arachidonic acid. Biochem J. 1998 Dec 15;336 ( Pt 3)(Pt 3):659-66.

[3]. T Köhler, et al. Phospholipase A2 inhibition by alkylbenzoylacrylic acids. Biochem Pharmacol. 1992 Aug 18;44(4):805-13.

物理化学性质

[ 密度 ]:
0.974 g/cm3

[ 沸点 ]:
550.8ºC at 760 mmHg

[ 分子式 ]:
C₂₈H₄₄O₃

[ 分子量 ]:
428.64700

[ 闪点 ]:
301ºC

[ 精确质量 ]:
428.32900

[ PSA ]:
54.37000

[ LogP ]:
8.31410

[ 外观性状 ]:
固体

[ 储存条件 ]:
2-8°C，密封，干燥

MSDS

详细MSDS(安全技术说明书)

安全信息

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

文献

Bile acid modulates transepithelial permeability via the generation of reactive oxygen species in the Caco-2 cell line.

Free Radic. Biol. Med. 39(6) , 769-80, (2005)

The barrier functions in epithelial and endothelial cells seem to be very important for maintaining normal biological homeostasis. However, it is unclear whether or how bile acids affect the epithelia...

Calcium entry in Trypanosoma brucei is regulated by phospholipase A2 and arachidonic acid.

Biochem. J. 336 ( Pt 3) , 659-66, (1998)

In contrast with mammalian cells, little is known about the control of Ca2+ entry into primitive protozoans. Here we report that Ca2+ influx in pathogenic Trypanosoma brucei can be regulated by phosph...

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