型号:
产品价格:电议      采购度:1601      原产地:美洲
发布时间:2021/7/24 0:57:53 所属地区:上海 上海市
简要描述:
Alendronate sodium hydrate 是一种 farnesyl diphosphate synthase 抑制剂,IC50 值为 460 nM。
标签:Fosamax
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CAS No. : 121268-17-5
MCE 站:Alendronate sodium hydrate
产品活性:Alendronate sodium hydrate 是一种 farnesyl diphosphate synthase 抑制剂,IC50 值为 460 nM。
研究领域:Others
作用靶点:Others
In Vitro: 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 [3H]mevalonolactone into proteins of 18-25 kDa and into nonsaponifiable lipids, including sterols in osteoclasts. Alendronate causes a dose-dependent inhibition of [3H]MVA incorporation into sterols and a concomitant increase in incorporation of radiolabel into IPP and DMAPP.
In Vivo: 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 delays 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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更新时间:2024/1/2 10:14:29
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