Alendronate sodium hydrate (Synonyms: 阿仑膦酸钠; Alendronate; MK 217; G-704650 Adronat)

目录号: HY-11101 纯度: 99.6%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Alendronate sodium hydrate 是一种 farnesyl diphosphate synthase 抑制剂，IC₅₀ 值为 460 nM。

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Alendronate sodium hydrate Chemical Structure

CAS No. : 121268-17-5

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规格	价格	是否有货
10 mM * 1 mL in Water	￥550	In-stock
100 mg	￥500	In-stock
500 mg	￥1600	In-stock
1 g		询价
5 g		询价

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Other Forms of Alendronate sodium hydrate:

Alendronic acid-d₆ In-stock
Alendronic acid In-stock
Alendronate-d₆ sodium hydrate 询价
Alendronate sodium 询价
Alendronate sodium hydrate (Standard) 询价

MCE 顾客使用本产品发表的 5 篇科研文献

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生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

Alendronate (sodium hydrate) is a farnesyl diphosphate synthase inhibitor with IC₅₀ of 460 nM.

IC₅₀ & Target

IC50: 460 nM (farnesyl diphosphate synthase)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
Lewis lung carcinoma cell line	IC₅₀	0.43 μM Compound: 4, alendronate	Cytotoxicity against mouse LLC cells after 24 hrs by resazurin assay Cytotoxicity against mouse LLC cells after 24 hrs by resazurin assay	[PMID: 21536448]
Lewis lung carcinoma cell line	IC₅₀	2.62 μM Compound: 4, alendronate	Cytotoxicity against mouse LLC cells after 72 hrs by resazurin assay Cytotoxicity against mouse LLC cells after 72 hrs by resazurin assay	[PMID: 21536448]

体外研究
(In Vitro)

Alendronate sodium hydrate 直接作用于破骨细胞，可抑制胆固醇生物合成途径中的限速步骤，这对破骨细胞功能至关重要^[1]。由于香叶基香叶基二磷酸水平降低，Alendronate sodium hydrate 抑制类异戊二烯生物合成途径并干扰蛋白质异戊二烯化。Alendronate sodium hydrate 抑制 [³H]mevalonolactone 掺入 18-25 kDa 的蛋白质和非皂化脂质，包括破骨细胞中的甾醇^[2]。Alendronate sodium hydrate 会剂量依赖性地抑制 [³H]MVA 掺入甾醇，并伴随增加放射性标记掺入 IPP 和 DMAPP^[3]。

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

体内研究
(In Vivo)

Alendronate sodium hydrate 引起兔胃糜烂，但不会引起大鼠胃窦溃疡。Alendronate sodium hydrate 增加了吲哚美辛诱发的胃窦溃疡的发生率和大小。Alendronate sodium hydrate 还会增强大鼠吲哚美辛引起的胃损伤，并延缓胃溃疡愈合^[4]。Alendronate sodium hydrate (0.04-0.1 mg/kg，每周两次或 0.1 mg/kg，每周) 部分阻断人 PC-3 ML 细胞骨转移的形成，并导致腹膜和其他软组织中的肿瘤形成。对小鼠进行 Alendronate sodium hydrate 预处理 (0.1 mg/kg，每周或每周两次) 并与紫杉醇一起给药 (10-50 mg/kg/天，每周两次或每周一次) 可阻断骨髓和软组织中 PC-3 ML 肿瘤的生长并将存活率显着提高 4-5 周^[5]。

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

Clinical Trial

分子量

325.12

Formula

C₄H₁₈NNaO₁₀P₂

CAS 号

121268-17-5

性状

固体

颜色

White to off-white

中文名称

阿仑膦酸钠

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

细胞实验：

H₂O 中的溶解度 : ≥ 28.57 mg/mL (87.88 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.0758 mL	15.3789 mL	30.7579 mL
5 mM	0.6152 mL	3.0758 mL	6.1516 mL
10 mM	0.3076 mL	1.5379 mL	3.0758 mL

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。

方案一

请依序添加每种溶剂： PBS
Solubility: 10 mg/mL (30.76 mM); 澄清溶液; 超声助溶 (<60°C)

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

计算结果

工作液所需浓度 : mg/mL

该产品水溶性佳，请具体参考实测水 / PBS / Saline 中的溶解度数据。

您所需的储备液浓度超过该产品的实测溶解度，如有需要，请与 MCE 中国技术支持联系。

纯度 & 产品资料

纯度: 99.6%

选择批次：

Data Sheet (647 KB) SDS (393 KB)

COA (246 KB) HNMR (110 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Fisher JE, et al. Alendronate mechanism of action: geranylgeraniol, an intermediate in the mevalonate pathway, prevents inhibition of osteoclast formation, bone resorption, and kinase activation in vitro. Proc Natl Acad Sci U S A. 1999 Jan 5;96(1):133-8 [Content Brief]

[2]. Bergstrom JD, et al. Alendronate is a specific, nanomolar inhibitor of farnesyl diphosphate synthase. Arch Biochem Biophys. 2000 Jan 1;373(1):231-41. [Content Brief]

[3]. Keller RK, et al. Mechanism of aminobisphosphonate action: characterization of alendronate inhibition of the isoprenoid pathway. Biochem Biophys Res Commun. 1999 Dec 20;266(2):560-3. [Content Brief]

[4]. Elliott SN, et al. Alendronate induces gastric injury and delays ulcer healing in rodents. Life Sci. 1998;62(1):77-91. [Content Brief]

[5]. Stearns ME, et al. Effects of alendronate and taxol on PC-3 ML cell bone metastases in SCID mice. Invasion Metastasis. 1996;16(3):116-31. [Content Brief]

Kinase Assay ^[3]	Rat liver cytosol is prepared from a separate piece of liver from rat. Assays are carried out in a total volume of 0.1 mL containing 10 mg of cytosolic protein, and components according to Rilling. All reaction components (except IPP) are mixed and kept on ice for 15 min. Reactions are initiated by the addition of [¹⁴C]IPP and incubation at 37°C. Reactions are stopped after 5 min by addition of 0.4 mL MeOH/HCl (4/1, by vol.) and the samples are incubated a further 15 min to hydrolyze the allylic pyrophosphates to petroleum ether-extractable products. Following addition of 0.5 mL water and 1 mL petroleum ether, 50% of the upper (petroleum ether-extractable) phase is taken for liquid scintillation analysis. Preliminary experiments indicated that the reaction is linear with time and protein under these conditions, and no more than 10% of the substrate is consumed. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Fisher JE, et al. Alendronate mechanism of action: geranylgeraniol, an intermediate in the mevalonate pathway, prevents inhibition of osteoclast formation, bone resorption, and kinase activation in vitro. Proc Natl Acad Sci U S A. 1999 Jan 5;96(1):133-8 [Content Brief] [2]. Bergstrom JD, et al. Alendronate is a specific, nanomolar inhibitor of farnesyl diphosphate synthase. Arch Biochem Biophys. 2000 Jan 1;373(1):231-41. [Content Brief] [3]. Keller RK, et al. Mechanism of aminobisphosphonate action: characterization of alendronate inhibition of the isoprenoid pathway. Biochem Biophys Res Commun. 1999 Dec 20;266(2):560-3. [Content Brief] [4]. Elliott SN, et al. Alendronate induces gastric injury and delays ulcer healing in rodents. Life Sci. 1998;62(1):77-91. [Content Brief] [5]. Stearns ME, et al. Effects of alendronate and taxol on PC-3 ML cell bone metastases in SCID mice. Invasion Metastasis. 1996;16(3):116-31. [Content Brief]

Kinase Assay
^[3]

Rat liver cytosol is prepared from a separate piece of liver from rat. Assays are carried out in a total volume of 0.1 mL containing 10 mg of cytosolic protein, and components according to Rilling. All reaction components (except IPP) are mixed and kept on ice for 15 min. Reactions are initiated by the addition of [¹⁴C]IPP and incubation at 37°C. Reactions are stopped after 5 min by addition of 0.4 mL MeOH/HCl (4/1, by vol.) and the samples are incubated a further 15 min to hydrolyze the allylic pyrophosphates to petroleum ether-extractable products. Following addition of 0.5 mL water and 1 mL petroleum ether, 50% of the upper (petroleum ether-extractable) phase is taken for liquid scintillation analysis. Preliminary experiments indicated that the reaction is linear with time and protein under these conditions, and no more than 10% of the substrate is consumed.

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

参考文献

[1]. Fisher JE, et al. Alendronate mechanism of action: geranylgeraniol, an intermediate in the mevalonate pathway, prevents inhibition of osteoclast formation, bone resorption, and kinase activation in vitro. Proc Natl Acad Sci U S A. 1999 Jan 5;96(1):133-8 [Content Brief]

[2]. Bergstrom JD, et al. Alendronate is a specific, nanomolar inhibitor of farnesyl diphosphate synthase. Arch Biochem Biophys. 2000 Jan 1;373(1):231-41. [Content Brief]

[3]. Keller RK, et al. Mechanism of aminobisphosphonate action: characterization of alendronate inhibition of the isoprenoid pathway. Biochem Biophys Res Commun. 1999 Dec 20;266(2):560-3. [Content Brief]

[4]. Elliott SN, et al. Alendronate induces gastric injury and delays ulcer healing in rodents. Life Sci. 1998;62(1):77-91. [Content Brief]

[5]. Stearns ME, et al. Effects of alendronate and taxol on PC-3 ML cell bone metastases in SCID mice. Invasion Metastasis. 1996;16(3):116-31. [Content Brief]

Alendronate sodium hydrate 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

H₂O	1 mM	3.0758 mL	15.3789 mL	30.7579 mL	76.8947 mL
	5 mM	0.6152 mL	3.0758 mL	6.1516 mL	15.3789 mL
	10 mM	0.3076 mL	1.5379 mL	3.0758 mL	7.6895 mL
	15 mM	0.2051 mL	1.0253 mL	2.0505 mL	5.1263 mL
	20 mM	0.1538 mL	0.7689 mL	1.5379 mL	3.8447 mL
	25 mM	0.1230 mL	0.6152 mL	1.2303 mL	3.0758 mL
	30 mM	0.1025 mL	0.5126 mL	1.0253 mL	2.5632 mL
	40 mM	0.0769 mL	0.3845 mL	0.7689 mL	1.9224 mL
	50 mM	0.0615 mL	0.3076 mL	0.6152 mL	1.5379 mL
	60 mM	0.0513 mL	0.2563 mL	0.5126 mL	1.2816 mL
	80 mM	0.0384 mL	0.1922 mL	0.3845 mL	0.9612 mL

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Alendronate sodium121268-17-5Alendronate MK 217 G-704650 Adronat阿仑膦酸钠MK217MK 217MK-217OthersInhibitorinhibitorinhibit

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Alendronate sodium hydrate (Synonyms: 阿仑膦酸钠; Alendronate; MK 217; G-704650 Adronat)

Customer Review

Other Forms of Alendronate sodium hydrate:

MCE 顾客使用本产品发表的 5 篇科研文献