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R59949
  • 品牌:chemstan
  • 产地:中国
  • 货号:CS-108355
  • cas:120166-69-0
  • 价格: ¥4800/mg
  • 发布日期: 2020-12-29
  • 更新日期: 2024-04-26
产品详请
产地 中国
品牌 chemstan
货号 CS-108355
用途范围 科研
英文名称 R59949
纯度 %
CAS编号 120166-69-0
规格 100 mg
分子式 C??H??F?N?OS
是否进口
Description

R59949 is a pan diacylglycerol kinase (DGK) inhibitor with an IC50 of 300 nM. R59949 strongly inhibits the activity of type I DGK α and γ and moderately attenuates the activity of type II DGK θ and κ. R59949 activates protein kinase C (PKC) by enhancing the levels of the endogenous ligand diacyl glycerol[1] [2] [3] .

In Vitro

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[1] .
In THP‐1 monocytes, R59949 attenuates CCL2‐evoked Ca2+ signalling with a half‐maximal concentration of 8.6 μM[2] .
R59949 inhibits inducible nitric oxide production through decreasing transplasmalemmal L-arginine uptake in vascular smooth muscle cells[4] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

489.58

Formula

C??H??F?N?OS

CAS No.

120166-69-0

SMILES

O=C1N(CCN2CC/C(CC2)=C(C3=CC=C(F)C=C3)\C4=CC=C(F)C=C4)C(NC5=C1C=CC=C5)=S

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
  • [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.


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