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抑制剂描述:

产品名称:Alendronate sodium hydrate

产品别名:见爱必信官网

英文别名:Alendronate sodium hydrate

靶点:SQS

CAS:121268-17-5

纯度:>98%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

Alendronate (Fosamax) is a farnesyl diphosphate synthase inhibitor with IC₅₀ of 460 nM. It is a nitrogen-containing bisphosphate that acts as a robust inhibitor of bone resorption and induces apoptosis in osteoclasts. It causes disruption of the ruffled border and actin cytoskeleton of osteoclasts and induces in vitro apoptosis of osteoclasts and macrophages by inhibiting farnesyl diphosphate synthase (IC₅₀ = 460 nM). It efficiently chelates metal ions and functions as a broad-spectrum MMP inhibitor (IC₅₀ ~ 40 - 70 uM). And it also displays antimetastatic, anti-invasive and cell-adhesion-promoting properties (IC₅₀ ~ 1 pM, in vitro invasion of prostate cancer cells).

溶解性:DMSO :20 mg/mL (61.3 mM) with gentle warming
Water :20 mg/mL (61.3 mM) with gentle warming

体外研究:

Alendronate, acting directly on osteoclasts, inhibits a rate-limiting step in the cholesterol biosynthesis pathway, essential for osteoclast function. Alendronate inhibits the isoprenoid biosynthesis pathway and interferes with protein prenylation, as a result of reduced geranylgeranyl diphosphate levels. Alendronate inhibits the incorporation of mevalonolactone into proteins of 18-25 kDa and into nonsaponifiable lipids, including sterols in osteoclasts. Alendronate causes a dose-dependent inhibition of MVA incorporation into sterols and a concomitant increase in incorporation of radiolabel into IPP and DMAPP.

体内研究:Alendronate causes erosions in the rabbit stomach, but not antral ulceration in rats. Alendronate increases the incidence and size of indomethacin-induced antral ulcers. Alendronate also enhances indomethacin-induced gastricdamage in the rat, and delayed gastric ulcer healing. Alendronate (0.04-0.1 mg/kg twice weekly or 0.1 mg/kg weekly) partially blocks the establishment of bone metastases by human PC-3 ML cells and results in tumor formation in the peritoneum and other soft tissues. Alendronate pretreatment of mice (0.1 mg/kg twice weekly or weekly) and dosing along with taxol (10-50 mg/kg/day, twice weekly, or weekly) blocks the growth of PC-3 ML tumors in the bone marrow and soft tissues in a statistically significant manner and improves survival rates significantly by 4-5 weeks.

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