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Alendronate sodium hydrate Sale

(Synonyms: 阿仑膦酸钠; Alendronate; MK 217; G-704650 Adronat) 目录号 : GC10348

An FPP synthase inhibitor

Alendronate sodium hydrate Chemical Structure

Cas No.:121268-17-5

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10mg
¥1,481.00
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500mg
¥1,586.00
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1g
¥2,342.00
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Sample solution is provided at 25 µL, 10mM.

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实验参考方法

Kinase experiment:

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.

References:

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

产品描述

Alendronate is an inhibitor of bone resorption with IC50 value of 2nM [1].

Alendronate is a bisphosphonate. It is developed as a therapeutic agent in many bone disorders such as osteoporosis as well as Paget's disease and tumoral bone disease. Alendronate inhibits the bone resorption through binding to bone mineral and subsequently preventing the osteoclasts from ingesting them. It not only affects the function of osteoclasts but also alter the morphology of the cells. In the in vitro assay, alendronate shows effective antiresorbing potency with IC50 value of 2nM when treated with osteoclast suspension. In organ culture, alendronate inhibits resorption by embryonic long bones and cultured calvaria [1, 2].

References:
[1] Sahni M, Guenther H L, Fleisch H, et al. Bisphosphonates act on rat bone resorption through the mediation of osteoblasts. Journal of Clinical Investigation, 1993, 91(5): 2004.
[2] Bell N H, Johnson R H. Bisphosphonates in the treatment of osteoporosis. Endocrine, 1997, 6(2): 203-206.

Chemical Properties

Cas No. 121268-17-5 SDF
别名 阿仑膦酸钠; Alendronate; MK 217; G-704650 Adronat
化学名 sodium hydrogen(4-amino-1-hydroxy-1-phosphonobutyl)phosphonate trihydrate
Canonical SMILES [O-]P(O[H])(C(O[H])(C([H])([H])C([H])([H])C([H])([H])N([H])[H])P(O[H])(O[H])=O)=O.[H]O[H].[H]O[H].[H]O[H].[Na+]
分子式 C4H18NNaO10P2 分子量 325.12
溶解度 ≥ 5.57mg/mL in Water 储存条件 Store at -20°C
General tips 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 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

制备储备液
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
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