Alendronate sodium hydrate 是 farnesyl diphosphate synthase 抑制剂(IC50:460 nM)。

Alendronate is a nitrogen-containing bisphosphonate, which is an effective inhibitor of bone resorption. It is utilized for the treatment and prevention of osteoporosis.

在小鼠中,一周一至两次0.1 mg/kg Alendronate预处理并联合使用10-50 mg/kg紫杉醇给药,可以阻断骨髓和软组织中PC-3 ML肿瘤的生长,并明显将生存时间提高到4-5周.在大鼠体内,Alendronate会增强吲哚美辛诱发的胃损伤,并延缓胃溃疡恢复.在兔子体内,Alendronate引起胃糜烂,同时增加吲哚美辛诱发的胃窦溃疡的发病率和面积.

阿仑膦酸钠,主要在破骨细胞中抑制胆固醇生物合成途径中的限速步骤。阿仑膦酸钠通过降低的香叶基香叶基二磷酸酯的水平,它可以干扰蛋白质异戊烯化,同时抑制类异戊二烯的生物合成途径。阿仑膦酸钠还以抑制0破骨细胞中的甾醇。

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.

121268-17-5

C4H18NNaO10P2

325.122

Alendronate sodium trihydrate;G-704650;Alendronate;阿仑膦酸钠;Fosamax;MK 217;G-704650 Adronat

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