Alendronate sodium hydrate (Synonyms: 阿侖膦酸鈉; Alendronate; MK 217; G-704650 Adronat)

目錄號(hào): HY-11101 純度: 99.6%: FAQs
Data Sheet SDS COA 產(chǎn)品使用指南

摩爾計(jì)算器

Alendronate sodium hydrate 是一種 farnesyl diphosphate synthase 抑制劑，IC₅₀ 值為 460 nM。

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Alendronate sodium hydrate Chemical Structure

CAS No. : 121268-17-5

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規(guī)格	價(jià)格	是否有貨
10 mM * 1 mL in Water	￥550	In-stock
100 mg	￥500	In-stock
500 mg	￥1600	In-stock
1 g		詢價(jià)
5 g		詢價(jià)

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Other Forms of Alendronate sodium hydrate:

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

MCE 顧客使用本產(chǎn)品發(fā)表的 5 篇科研文獻(xiàn)

•J Med Chem. 2024 Aug 26. [Abstract]
•Cell Rep. 2022 Oct 25;41(4):111508. [Abstract]
•Int J Mol Sci. 2024 Jul 16;25(14):7798. [Abstract]
•Am J Physiol Endocrinol Metab. 2024 May 8. [Abstract]
•J Biol Chem. 2019 Jul 19;294(29):11240-11247. [Abstract]

Alendronate sodium hydrate 相關(guān)產(chǎn)品

•相關(guān)化合物庫(kù):

•同靶點(diǎn)產(chǎn)品:

•同靶點(diǎn)蛋白產(chǎn)品:

生物活性
實(shí)驗(yàn)參考方法
純度 & 產(chǎn)品資料
參考文獻(xiàn)

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)

細(xì)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]

體外研究
(In Vitro)

Alendronate sodium hydrate 直接作用于破骨細(xì)胞，可抑制膽固醇生物合成途徑中的限速步驟，這對(duì)破骨細(xì)胞功能至關(guān)重要^[1]。由于香葉基香葉基二磷酸水平降低，Alendronate sodium hydrate 抑制類異戊二烯生物合成途徑并干擾蛋白質(zhì)異戊二烯化。Alendronate sodium hydrate 抑制 [³H]mevalonolactone 摻入 18-25 kDa 的蛋白質(zhì)和非皂化脂質(zhì)，包括破骨細(xì)胞中的甾醇^[2]。Alendronate sodium hydrate 會(huì)劑量依賴性地抑制 [³H]MVA 摻入甾醇，并伴隨增加放射性標(biāo)記摻入 IPP 和 DMAPP^[3]。

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

體內(nèi)研究
(In Vivo)

Alendronate sodium hydrate 引起兔胃糜爛，但不會(huì)引起大鼠胃竇潰瘍。Alendronate sodium hydrate 增加了吲哚美辛誘發(fā)的胃竇潰瘍的發(fā)生率和大小。Alendronate sodium hydrate 還會(huì)增強(qiáng)大鼠吲哚美辛引起的胃損傷，并延緩胃潰瘍愈合^[4]。Alendronate sodium hydrate (0.04-0.1 mg/kg，每周兩次或 0.1 mg/kg，每周) 部分阻斷人 PC-3 ML 細(xì)胞骨轉(zhuǎn)移的形成，并導(dǎo)致腹膜和其他軟組織中的腫瘤形成。對(duì)小鼠進(jìn)行 Alendronate sodium hydrate 預(yù)處理 (0.1 mg/kg，每周或每周兩次) 并與紫杉醇一起給藥 (10-50 mg/kg/天，每周兩次或每周一次) 可阻斷骨髓和軟組織中 PC-3 ML 腫瘤的生長(zhǎng)并將存活率顯著提高 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 號(hào)

121268-17-5

性狀

固體

顏色

White to off-white

中文名稱

阿侖膦酸鈉

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)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)

溶解性數(shù)據(jù)

細(xì)胞實(shí)驗(yàn)：

H₂O 中的溶解度 : ≥ 28.57 mg/mL (87.88 mM)

* "≥" means soluble, but saturation unknown.

配制儲(chǔ)備液

濃度溶劑體積質(zhì)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

查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

* 備注：如您選擇水作為儲(chǔ)備液，請(qǐng)稀釋至工作液后，再用 0.22 μm 的濾膜過(guò)濾除菌后使用。

摩爾計(jì)算器
稀釋計(jì)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

濃度 _(start)

體積 _(start)

濃度 _(final)

體積 _(final)

動(dòng)物實(shí)驗(yàn)：

以下溶解方案，請(qǐng)直接配制工作液。建議現(xiàn)用現(xiàn)配，在短期內(nèi)盡快用完。以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶。

方案一

請(qǐng)依序添加每種溶劑： PBS
Solubility: 10 mg/mL (30.76 mM); 澄清溶液; 超聲助溶 (<60°C)

動(dòng)物溶解方案計(jì)算器

請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只

由于實(shí)驗(yàn)過(guò)程有損耗，建議您多配一只動(dòng)物的量

計(jì)算結(jié)果

工作液所需濃度 : mg/mL

該產(chǎn)品水溶性佳，請(qǐng)具體參考實(shí)測(cè) 水 / PBS / Saline 中的溶解度數(shù)據(jù)。

您所需的儲(chǔ)備液濃度超過(guò)該產(chǎn)品的實(shí)測(cè)溶解度，如有需要，請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。

純度 & 產(chǎn)品資料

純度: 99.6%

選擇批次：

Data Sheet (647 KB) SDS (393 KB)

COA (269 KB) HNMR (110 KB)

產(chǎn)品使用指南 (1538 KB)

參考文獻(xiàn)

[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.
參考文獻(xiàn)	[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.

參考文獻(xiàn)

[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 相關(guān)分類

完整儲(chǔ)備液配制表

可選溶劑	濃度溶劑體積質(zhì)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

* 備注：如您選擇水作為儲(chǔ)備液，請(qǐng)稀釋至工作液后，再用 0.22 μm 的濾膜過(guò)濾除菌后使用。

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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阿侖膦酸鈉MK217MK 217MK-217OthersInhibitorinhibitorinhibit

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Alendronate sodium hydrate (Synonyms: 阿侖膦酸鈉; Alendronate; MK 217; G-704650 Adronat)

Customer Review

Other Forms of Alendronate sodium hydrate:

MCE 顧客使用本產(chǎn)品發(fā)表的 5 篇科研文獻(xiàn)