Powder: -20°C for 3 years | In solvent: -80°C for 1 year
NE 10790 (3-PEHPC) 是一种二磷酸利塞磷酸盐的磷酸酯类似物,是一种法尼焦磷酸合成酶的弱抑制剂,也是一种弱抗吸收剂。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 859 | 现货 | ||
5 mg | ¥ 2,310 | 现货 | ||
10 mg | ¥ 3,630 | 现货 | ||
25 mg | ¥ 5,890 | 现货 | ||
50 mg | ¥ 8,160 | 现货 | ||
100 mg | ¥ 10,800 | 现货 |
产品描述 | NE 10790 (3-PEHPC) is a phosphonocarboxylate analogue of the potent bisphosphonate risedronate and is a weak anti-resorptive agent. Although NE10790 was a poor inhibitor of FPP synthase |
体外活性 | NE 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[1]. |
别名 | 3-PEHPC |
分子量 | 247.14 |
分子式 | C8H10NO6P |
CAS No. | 152831-36-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: 5 mg/mL (20.23 mM), when pH is adjusted to 6 with NaOH. Sonification is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
H2O | 1 mM | 4.0463 mL | 20.2314 mL | 40.4629 mL | 101.1572 mL |
5 mM | 0.8093 mL | 4.0463 mL | 8.0926 mL | 20.2314 mL | |
10 mM | 0.4046 mL | 2.0231 mL | 4.0463 mL | 10.1157 mL | |
20 mM | 0.2023 mL | 1.0116 mL | 2.0231 mL | 5.0579 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
NE 10790 152831-36-2 Others inhibit 3-PEHPC NE10790 Inhibitor NE-10790 inhibitor