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R59949

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Chemical Structure| 120166-69-0 同义名 : Diacylglycerol Kinase Inhibitor II;DKGI-II
CAS号 : 120166-69-0
货号 : A701829
分子式 : C28H25F2N3OS
纯度 : 99%+
分子量 : 489.579
MDL号 : MFCD00069258
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(214.47 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 R59949 is a pan diacylglycerol kinase (DGK) inhibitor with an IC50 value of 300 nM. R59949 strongly inhibits type I DGK α and γ activity, and moderately attenuates type II DGK θ and κ activity. R59949 activates PKC by increasing the levels of the endogenous ligand diacylglycerol[1][2][3]. .In the presence of R59949, vasopressin as well as collagen-induced release reactions and aggregation are strongly increased, independent of the formation of arachidonic acid metabolites[1].In THP-1 monocytes, R59949 attenuates CCL2-induced Ca2+ signalling at a half-maximal concentration of 8.6 μM[2].R59949 inhibits inducible nitric oxide production by reducing transplasma membrane L-arginine uptake in vascular smooth muscle cells[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.04mL

0.41mL

0.20mL

10.21mL

2.04mL

1.02mL

20.43mL

4.09mL

2.04mL
参考文献

[1]de Chaffoy de Courcelles D, et al. The role of endogenously formed diacylglycerol in the propagation and termination of platelet activation. A biochemical and functional analysis using the novel diacylglycerol kinase inhibitor, R 59 949. J Biol Chem. 1989;264(6):3274-3285.

[2]Day P, et al. Inhibitors of DAG metabolism suppress CCR2 signalling in human monocytes. Br J Pharmacol. 2019;176(15):2736-2749.

[3]Meinhardt G, et al. Effect of novel modulators of protein kinase C activity upon chemotherapy-induced differentiation and apoptosis in myeloid leukemic cells. Anticancer Drugs. 2002;13(7):725-733.

[4]Shimomura T, et al. R59949, a diacylglycerol kinase inhibitor, inhibits inducible nitric oxide production through decreasing transplasmalemmal L-arginine uptake in vascular smooth muscle cells. Naunyn Schmiedebergs Arch Pharmacol. 2017;390(2):207-214.