Zoledronic Acid 是一种含氮二磷酸盐，能抑制破骨细胞的分化和凋亡，具有高效的抗骨质再吸收活性，也有抗癌作用。

Zoledronate is a bisphosphonate. Zometa is used to prevent skeletal fractures in patients with cancers such as multiple myeloma and prostate cancer. It can also be used to treat hypercalcemia of malignancy and can be helpful for treating pain from bone metastases. An annual dose of Zoledronate may also prevent recurring fractures in patients with a previous hip fracture. Zoledronate is a single 5 mg infusion for the treatment of Paget's disease of bone. In 2007, the FDA also approved Reclast for the treatment of postmenopausal osteoporosis.

Zoledronic acid（120 mg/kg,皮下注射）预防5T2 mM小鼠中损伤的形成,防止松质骨损失和骨矿物质密度的丧失,并减少破骨细胞周长,也降低副蛋白浓度和肿瘤负荷,并减少血管生成.

Zoledronic acid在浓度为0.1–10 μM时对MDA-MB-231细胞几乎没有影响,然而在100 μM浓度下会导致细胞数量明显减少。10 μM Zoledronic acid会导致MCF-7细胞凋亡增加超过四倍,而在100 μM浓度下,诱导细胞凋亡的比例增加6倍。与单独使用唑来膦酸（155.71％）相比,唑来膦酸（10 μM）和紫杉醇（2 μM）导致细胞凋亡增加5倍（对照组为774.8％）,比单用紫杉醇增加4倍（189.68％）。10 μM和100 μM Zoledronic acid导致MCF-7细胞的比例显著降低（分别为对照的49.54％和23.55％）（P<0.05）。100 μM Zoledronic acid在72小时时会引起MCF-7细胞数减少63.5%,在96小时时,会使其减少87.1%。Zoledronic acid诱导的MCF-7乳腺癌细胞凋亡会被甲羟戊酸途径中间体的加入所抑制,这与在破骨细胞,巨噬细胞和骨髓瘤细胞中的情况相一致。Zoledronic acid防止糖皮质激素地塞米松对人成骨细胞中OPG mRNA和蛋白质产生的抑制作用。Zoledronic acid在人类成骨细胞中分别诱导2倍的I型胶原分泌和4倍的碱性磷酸酶活性。Zoledronic acid剂量依赖性增强OPG基因的表达和人类成骨细胞中蛋白质的分泌,在10 nM浓度下,72小时后具有最大效果,这与Zoledronic acid更高的生物学效能相一致。

118072-93-8

C5H10N2O7P2

272.09

唑来膦酸;CGP42446A;ZOL 446;CGP-4244;CGP 42446;Zometa;Zoledronate

1.1eq. NaOH:13.6 mg/mL (50 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years