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2-(对戊基桂皮酰基)胺-4-氯代苯甲酸

2-(对戊基桂皮酰基)胺-4-氯代苯甲酸用途

ONO-RS-082是磷脂酶A(PLA)的抑制剂[1]。ONO-RS-082以1.0μM的IC50抑制PLA2,但即使在100μM时也不抑制PLC[2]。

2-(对戊基桂皮酰基)胺-4-氯代苯甲酸名称

[ CAS 号 ]:
99754-06-0

[ 中文名 ]:
2-(对戊基桂皮酰基)胺-4-氯代苯甲酸

[ 英文名 ]:
ONO-RS-082

[中文别名 ]:

2-(对肉桂酰戊酯)氨基-4-氯苯甲酸

[英文别名 ]:

Ono-RS-082
C21H22ClNO3

2-(对戊基桂皮酰基)胺-4-氯代苯甲酸生物活性

[ 描述 ]:

ONO-RS-082是磷脂酶A(PLA)的抑制剂[1]。ONO-RS-082以1.0μM的IC50抑制PLA2,但即使在100μM时也不抑制PLC[2]。

[ 相关类别 ]:

信号通路 >> 代谢酶/蛋白酶 >> 磷脂

研究领域 >> 炎症/免疫

[体外研究]

ONO-RS-082(10μM)可防止铜绿假单胞菌菌株PAO1诱导的多形核细胞(PMN)跨上皮迁移,表明PLA2活性对这一过程至关重要[3]。细胞活力测定[3]细胞系：A549肺上皮细胞系浓度：10μM孵育时间：2小时预处理结果：完全阻断HXA3介导的PAO1诱导的PMN跨上皮迁移。在很大程度上阻止了PAO1诱导的PGE2释放。

[体内研究]

ONO-RS-082在体内长期激活KCNK3(50 mg/kg/天；预防性治疗,第0天至第21天)可减少MCT-PH模型中PH值的发展[4]。相比之下,通过ONO-RS-082(治疗性治疗)在体内短期激活KCNK3无法减轻PH症状,这是由于MCT-PH大鼠在第14至21天时KCNK3表达完全丧失[4]。动物模型：MCT-肺动脉高压(PH)大鼠模型[4]剂量：50 mg/kg/天给药：结果：长期降低MCT-PH模型中PH的发展。

[参考文献]

[1]. H S Banga,et al. Activation of phospholipases A and C in human platelets exposed to epinephrine: role of glycoproteins IIb/IIIa and dual role of epinephrine. Proc Natl Acad Sci U S A.1986 Dec;83(23):9197-201.

[2]. H Ohno, et al. Effect of phospholipase A2 inhibitors on mouse T lymphocytes. I. Phospholipase A2 inhibitors exert similar immunological activities as glycosylation inhibiting factor. Int Immunol. 1989;1(4):425-33.

[3]. Bryan P Hurley, et al. Selective eicosanoid-generating capacity of cytoplasmic phospholipase A2 in Pseudomonas aeruginosa-infected epithelial cells. Am J Physiol Lung Cell Mol Physiol. 2011 Feb;300(2):L286-94.

[4]. Hélène Le Ribeuz, et al. Implication of Potassium Channels in the Pathophysiology of Pulmonary Arterial Hypertension. Biomolecules. 2020 Sep 1;10(9):1261.

2-(对戊基桂皮酰基)胺-4-氯代苯甲酸物理化学性质

[ 密度 ]:
1.247g/cm3

[ 沸点 ]:
580.5ºC at 760mmHg

[ 分子式 ]:
C₂₁H₂₂ClNO₃

[ 分子量 ]:
371.85700

[ 闪点 ]:
304.9ºC

[ 精确质量 ]:
371.12900

[ PSA ]:
66.40000

[ LogP ]:
5.49580

[ 折射率 ]:
1.633

[ 储存条件 ]:
-20°C，密闭，干燥

2-(对戊基桂皮酰基)胺-4-氯代苯甲酸MSDS

详细MSDS(安全技术说明书)

2-(对戊基桂皮酰基)胺-4-氯代苯甲酸安全信息

[ 符号 ]:

GHS09

[ 信号词 ]:
Warning

[ 危害声明 ]:
H410

[ 警示性声明 ]:
P273-P501

[ 危险品运输编码 ]:
UN 3077 9 / PGIII

2-(对戊基桂皮酰基)胺-4-氯代苯甲酸文献

Role of phospholipase A(2) in retrograde transport of ricin.

Toxins (Basel.) 3(9) , 1203-19, (2011)

Ricin is a protein toxin classified as a bioterror agent, for which there are no known treatment options available after intoxication. It is composed of an enzymatically active A-chain connected by a ...

A role for phospholipase A2 activity in membrane tubule formation and TGN trafficking.

Traffic 11(12) , 1530-6, (2010)

We have investigated the role of phospholipase A(2) (PLA(2) ) enzymes in generating membrane tubules at the trans-Golgi network (TGN). Constitutive TGN membrane tubules and those induced by over-expre...

Pyrimidine nucleotide-stimulated thromboxane A2 release from cultured glia.

Cell. Mol. Neurobiol. 18(5) , 477-86, (1998)

1. Uridine triphosphate (UTP), uridine diphosphate (UDP), cytidine triphosphate (CTP), and deoxythymidine triphosphate (TTP) caused concentration-dependent increases in the release of thromboxane A2 (...

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