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NE 10790

产品编号 T16289 CAS 152831-36-2

别名: 3-PEHPC

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。

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NE 10790, CAS 152831-36-2

规格	价格/CNY	货期
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

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生物活性

化学信息

存储 & 溶解度

参考文献

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

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

H2O: 5 mg/mL (20.23 mM), when pH is adjusted to 6 with NaOH. Sonification is recommended.

溶液配制表

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

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

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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. 2. Hald A , Hansen R R , Thomsen M W , et al. Cancer-induced bone loss and associated pain-related behavior is reduced by risedronate but not its phosphonocarboxylate analog NE-10790[J]. 2009, 125(5):1177-1185.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

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。

第一步：请输入动物实验的基本信息

剂量

mg/kg

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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