货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
T29175-1ml	10mM in DMSO	￥670.00 T29175-1ml ￥670.00 3-5天	0 货期：3-5天	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

T29175-1ml

10mM in DMSO

￥670.00

货期：3-5天

产品描述：

R59949是一种二酰基甘油激酶（diacylglycerol kinase, DGK）抑制剂，通过减少血管平滑肌细胞中跨质体 L-精氨酸摄取来抑制诱导型一氧化氮的产生。R59949 强烈抑制 I 型 DGK α和γ的活性，并适度减弱 II 型 DGK θ和κ的活性

靶点：

DKG:0.3 μM

体外研究：

In the presence of R59949, vasopressin- as well as collagen-induced release reaction and aggregation was strongly increased, independently of the formation of arachidonate metabolites.

In THP‐1 monocytes, R59949 attenuates CCL2‐evoked Ca2+ signalling with a half‐maximal concentration of 8.6 μM.

R59949 inhibits inducible nitric oxide production through decreasing transplasmalemmal L-arginine uptake in vascular smooth muscle cells.

体内研究：

R59949 upregulates the expression of PHD-2, also downregulates HIF-1α and vascular endothelial growth factor (VEGF) in the retina of oxygen-induced retinopathy (OIR) mice, suggesting a potential possibility that R59949 suppresses retinal neovascular pathophysiology via PHD2/HIF-1α/VEGF pathway

细胞实验：

Cell lines: rat aortic smooth muscle cells (RASMCs) Concentrations: 10 µM Incubation Time: 30 min Method: RASMCs are prepared from adult male Wistar rats and cultured in DMEM containing 10% FBS under 5% CO2 at 37 ℃. Cultured cells showing a confluent condition in a 24-well plate are used for experiments. The cells are pretreated with R59949 at 10 μM or cycloheximide at 1 μM at 30 min before stimulation with IL-1β at 10 ng/ml or a vehicle for 24 h. Measurement of NOX is performed in the presence of nitrate reductase using a commercial kit. After incubation with nitrate reductase at room temperature for 2 h, aliquots of the culture medium are mixed with Griess reagent (1% sulphanilamide/0.1% N-(1-naphthyl) ethylenediamine dihydrochloride in 5% phosphoric acid). The mixture is then incubated at room temperature for 10 min, and its absorbance is measured at 540 nm using a photometer.

动物实验：

Animal Models: C57BL/6J mice Dosages: 10 μg/g/day Administration: i.p.

参考文献：

1. Shimomura T, et al. Naunyn Schmiedebergs Arch Pharmacol. 2017 Feb;390(2):207-214. 2. Yang L, et al. J Mol Neurosci. 2015 May;56(1):78-88.

溶解性：

Soluble in DMSO、Ethanol

保存条件：

-80℃（运输条件：冰袋低温运输）

备注：

R59949 是一种泛二酰甘油激酶 (DGK) 抑制剂，IC50 为 300 nM。R59949 强烈抑制 Ⅰ 型 DGKα 和 γ 的活性，中度减弱 Ⅱ 型 DGKθ 和 κ 的活性。R59949 通过提高内源性配体二酰甘油水平来激活蛋白激酶C (PKC)。

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.043 ml	10.213 ml	20.426 ml
5 mM	0.409 ml	2.043 ml	4.085 ml
10 mM	0.204 ml	1.021 ml	2.043 ml
50 mM	0.041 ml	0.204 ml	0.409 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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