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R59949

Cat. No.:YN310401

  • CAS No. :120166-69-0

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    • 参考文献
    • 产品名称: R59949
      CAS No.: 120166-69-0
      Chemical Name: 3-[2-[4-[bis(4-fluorophenyl)methylene]-1-piperidinyl]ethyl]-2,3-dihydro-2-thioxo-4(1H)-quinazolinone
      Synonyms:R59949;R 59949
      分子量:489.6
      分子式:C28H25F2N3OS
      SMILES:S=C1N(CCN2CC/C(CC2)=C(C3=CC=C(F)C=C3)/C4=CC=C(F)C=C4)C(C5=CC=CC=C5N1)=O
      存储:Please store the product under the recommended conditions in theCertificate of Analysis.
      运输:Room temperature in continental US; may vary elsewhere.
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      Purity: 98%
    • 产品描述: 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)。
      IC50和靶点:
      In Vitro:
      In Vivo:
      Clinical Trial:
      Solvent & Solubility:
    • de Chaffoy de Courcelles, D., Roevens, P., Van Belle, H., 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 949J. Biol. Chem.264(6),3274-3285(1989)

      Du, X., Jiang, Y., Qian, W., et al.Fatty acids inhibit growth-factor-induced diacylglycerol kinase alpha activation in vascular smooth-muscle cellsBiochem J.357(Pt. 1),275-282(2001)

      Kurohane Kaneko, Y., Kobayashi, Y., Motoki, K., et al.Depression of type I diacylglycerol kinases in pancreatic β-cells from male mice results in impaired insulin secretionEndocrinology154(11),4089-4098(2013)

      Yang, L., Xu, Y., Li, W., et al.Diacylglycerol kinase (DGK) inhibitor II (R59949) could suppress retinal neovascularization and protect retinal astrocytes in an oxygen-induced retinopathy modelJ. Mol. Neurosci.56(1),78-88(2015)

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