Alendronate sodium hydrate

An FPP synthase inhibitor

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10mg

￥1787.00

1430.00

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500mg

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1g

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货号: ajci4938
CAS: 121268-17-5
别名: 阿仑膦酸钠; Alendronate; MK 217; G-704650 Adronat
分子式: C4H18NNaO10P2
分子量: 325.12
纯度: >98%
溶解度: ≥ 5.57mg/mL in Water
储存: Store at -20°C
库存: 现货

Background

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].

参考文献:
[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.

Protocol

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.

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
[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.