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NE 10790

CAS No. 152831-36-2

NE 10790 ( 3-PEHPC )

产品货号. M22004 CAS No. 152831-36-2

NE 10790 is a phosphonocarboxylate analogue of the potent bisphosphonate risedronate and is a weak anti-resorptive agent.

纯度: >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
规格 价格/人民币 库存 数量
5MG ¥1847 有现货
10MG ¥3013 有现货
25MG ¥5095 有现货
50MG ¥7258 有现货
100MG ¥9882 有现货
200MG 获取报价 有现货
500MG 获取报价 有现货
1G 获取报价 有现货

生物学信息

  • 产品名称
    NE 10790
  • 注意事项
    本公司产品仅用于科研实验,不得用于人体或动物的临床与诊断
  • 产品简述
    NE 10790 is a phosphonocarboxylate analogue of the potent bisphosphonate risedronate and is a weak anti-resorptive agent.
  • 产品描述
    NE 10790 is a phosphonocarboxylate analogue of the potent bisphosphonate risedronate and is a weak anti-resorptive agent. Although NE10790 was a poor inhibitor of FPP synthaseNE 10790 did inhibit prenylation in J774 macrophages and osteoclasts, but only of proteins of molecular mass approximately 22-26 kDa, the prenylation of which was not affected by peptidomimetic inhibitors of either farnesyl transferase (FTI-277) or geranylgeranyl transferase I (GGTI-298).?These 22-26-kDa proteins were shown to be geranylgeranylated by labelling J774 cells with [(3)H]geranylgeraniol.?Furthermore, NE10790 inhibited incorporation of [(14)C]mevalonic acid into Rab6, but not into H-Ras or Rap1, proteins that are modified by FTase and GGTase I, respectively.?These data demonstrate that NE10790 selectively prevents Rab prenylation in intact cells.?In accord, NE10790 inhibited the activity of recombinant Rab GGTase in vitro, but did not affect the activity of recombinant FTase or GGTase I. NE10790 therefore appears to be the first specific inhibitor of Rab GGTase to be identified.?In contrast to risedronate, NE10790 inhibited bone resorption in vitro without markedly affecting osteoclast number or the F-actin "ring" structure in polarized osteoclasts.?However, NE10790 did alter osteoclast morphology, causing the formation of large intracellular vacuoles and protrusion of the basolateral membrane into large, "domed" structures that lacked microvilli.?The anti-resorptive activity of NE10790 is thus likely due to disruption of Rab-dependent intracellular membrane trafficking in osteoclasts.
  • 同义词
    3-PEHPC
  • 通路
    Others
  • 靶点
    Other Targets
  • 受体
    FPP synthase
  • 研究领域
    ——
  • 适应症
    ——

化学信息

  • CAS Number
    152831-36-2
  • 分子量
    247.14
  • 分子式
    C8H10NO6P
  • 纯度
    >98% (HPLC)
  • 溶解度
    H2O:5 mg/mL (20.23 mM; ultrasonic and adjust pH to 6 with NaOH)
  • SMILES
    OC(=O)C(O)(CC1=CN=CC=C1)P(O)(O)=O
  • 化学全称
    ——

运输与储存

  • 储存条件
    (-20℃)
  • 运输条件
    With Ice Pack
  • 稳定性
    ≥ 2 years

参考文献

1. Coxon FP, et al. Identification of a novel phosphonocarboxylate inhibitor of Rab geranylgeranyl transferase that specifically prevents Rab prenylation in osteoclasts and macrophages. J Biol Chem. 2001 Dec 21;276(51):48213-22.
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