二乙酰基甘油激酶

二乙酰基甘油激酶用途

R 59-022 (DKGI-I) 是一种二酰甘油激酶 (diacylglycerol kinase) 抑制剂 (IC50=2.8 μM)。R 59-022 是一种 5-HTR 拮抗剂,激活蛋白激酶 C (PKC)。R 59-022 增强凝血酶诱导血小板产生二酰甘油和抑制中性粒细胞产生磷脂酸。

二乙酰基甘油激酶名称

[ CAS 号 ]:
93076-89-2

[ 中文名 ]:
二乙酰基甘油激酶

[ 英文名 ]:
R 59-022

[英文别名 ]:

R 59022

二乙酰基甘油激酶生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 表观遗传学 >> PKC

研究领域 >> 感染

研究领域 >> 炎症/免疫

研究领域 >> 神经疾病

信号通路 >> TGF-beta/Smad 信号通路 >> PKC

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 5-HT受体

信号通路 >> 神经信号通路 >> 5-HT受体

[体外研究]

在完整的血小板中,R 59-022能够在甘油二酯水平上阻断凝血酶诱导的肌醇脂质循环,并导致蛋白激酶C活性升高[1]。R 59－022(10μm)有利于聚集,而不是由凝血酶次最大浓度引起的形状变化。R59022(10μM)对凝血酶在细胞外Ca2+存在或不存在时动员细胞内Ca2+的剂量-反应曲线均无显著影响。R 59-022是一种丝状病毒进入的抑制剂,可阻止丝状病毒颗粒的大细胞摄取,抑制多个丝状病毒GPs介导的进入,并阻止复制性EBOV生长。R 59-022以浓度依赖的方式阻断EBOV假型的进入(IC50：~5μM)。R 59-022携带EBOV GP的vlp进入剂量依赖性降低(IC50：~2μM)。R 59-022(2-12μM；1小时)可抑制EBOV-GP介导的多种细胞进入。R 59-022(5μM；30分钟)阻断vero细胞中的大细胞增生[5]。

[参考文献]

[1]. de Chaffoy de Courcelles DC, et al. R 59 022, a diacylglycerol kinase inhibitor. Its effect on diacylglycerol and thrombin-induced C kinase activation in the intact platelet. J Biol Chem. 1985 Dec 15;260(29):15762-70.

[2]. Nunn DL, et al. A diacylglycerol kinase inhibitor, R59022, potentiates secretion by and aggregation of thrombin-stimulated human platelets. Biochem J. 1987 May 1;243(3):809-13.

[3]. Jones JA, et al. Influence of phorbol esters, and diacylglycerol kinase and lipase inhibitors on noradrenalinerelease and phosphoinositide hydrolysis in chromaffin cells. Br J Pharmacol. 1990 Nov;101(3):521-6.

[4]. Boroda S, et al. Dual activities of ritanserin and R59022 as DGKα inhibitors and serotonin receptor antagonists. Biochem Pharmacol. 2017 Jan 1;123:29-39.

[5]. Stewart CM, et al. A Diacylglycerol Kinase Inhibitor, R-59-022, Blocks Filovirus Internalization in Host Cells. Viruses. 2019 Mar 1;11(3). pii: E206.

二乙酰基甘油激酶物理化学性质

[ 密度 ]:
1.26g/cm3

[ 沸点 ]:
619.8ºC at 760mmHg

[ 分子式 ]:
C₂₇H₂₆FN₃OS

[ 分子量 ]:
459.57800

[ 闪点 ]:
328.6ºC

[ 精确质量 ]:
459.17800

[ PSA ]:
65.85000

[ LogP ]:
5.28180

[ 折射率 ]:
1.654

[ 储存条件 ]:
-20°C，惰性气体保存

二乙酰基甘油激酶安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危害码 (欧洲) ]:
Xi

[ 安全声明 (欧洲) ]:
S23-S24/25

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

二乙酰基甘油激酶文献

Diacylglycerol kinase epsilon in bovine and rat photoreceptor cells. Light-dependent distribution in photoreceptor cells.

Exp. Eye Res. 112 , 139-50, (2013)

The present study shows the selective light-dependent distribution of 1,2-diacylglycerol kinase epsilon (DAGKɛ) in photoreceptor cells from bovine and albino rat retina. Immunofluorescence microscopy ...

Insulin action on polyunsaturated phosphatidic acid formation in rat brain: an "in vitro" model with synaptic endings from cerebral cortex and hippocampus.

Neurochem. Res. 34(7) , 1236-48, (2009)

The highly efficient formation of phosphatidic acid from exogenous 1-stearoyl-2-arachidonoyl-sn-glycerol (SAG) in rat brain synaptic nerve endings (synaptosomes) from cerebral cortex and hippocampus i...

The role of diacylglycerol as a modulator of oxytocin-stimulated phasic contractions in myometrium from pregnant and nonpregnant rats.

Am. J. Obstet. Gynecol. 182(4) , 943-9, (2000)

The role of diacylglycerol in the phosphatidylinositol-signaling pathway is to activate protein kinase C. In the myometrium, protein kinase C activation leads to inhibition of phasic contractions. The...

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