Zoledronic Acid是一种第三代含氮双膦酸盐类骨吸收抑制剂。
Cas No.:118072-93-8
Sample solution is provided at 25 µL, 10mM.
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Zoledronic Acid is a third-generation nitrogen-containing bisphosphonate bone resorption inhibitor. Zoledronic Acid reduces bone calcium release and lowers blood calcium levels by inhibiting osteoclast activity and inducing osteoclast apoptosis. Zoledronic Acid blocks the mevalonate pathway by inhibiting farnesyl pyrophosphate synthase activity. Zoledronic Acid can be used in research related to osteoporosis, Paget's disease, bone metastases of malignant tumors, and hypercalcemia caused by malignant tumors[1-4].
In vitro, CT26 colon cancer cells were treated with Zoledronic Acid (0-300μM) for 24-48 hours. Zoledronic Acid inhibited cell proliferation, induced apoptosis, and regulated autophagy[5]. Under high glucose conditions, MC3T3-E1 cells were treated with Zoledronic Acid (1mM) for 7 days. Zoledronic Acid significantly upregulated the expression of RUNX2, miR-133, and miR-204, while downregulating the expression of MALAT1 and miR-20a[6].
In vivo, female Balb/c mice were subcutaneously injected with Zoledronic Acid (5μg/kg) every other day for 10 days. Zoledronic Acid prevented carboplatin-induced bone loss and muscle weakness[7]. Male C57BL/6J mice received a single subcutaneous injection of Zoledronic Acid (100μg/kg). Zoledronic Acid increased body weight and muscle mass, improved muscle structural damage, increased the proportion of type I muscle fibers, and upregulated the protein expression of β-catenin and AKT, as well as the mRNA expression of Wnt3a, Wnt16, Myf5, and PI3K[8].
References:
[1] Cheer SM, Noble S. Zoledronic acid. Drugs. 2001;61(6):799-805; discussion 806.
[2] Finianos A, Aragon-Ching JB. Zoledronic acid for the treatment of prostate cancer. Expert Opin Pharmacother. 2019 Apr;20(6):657-666.
[3] Karpuz S. Zoledronic acid-induced severe lymphopenia. Osteoporos Int. 2023 Sep;34(9):1653-1655.
[4] Ishikawa T. Differences between zoledronic acid and denosumab for breast cancer treatment. J Bone Miner Metab. 2023 May;41(3):301-306.
[5] Zhu J, Liu M, Liu Y, et al. Zoledronic Acid Regulates Autophagy and Induces Apoptosis in Colon Cancer Cell Line CT26. Biomed Res Int. 2017;2017:7203584.
[6] Chen HL, Hu JP, Li JF, et al. Zoledronic acid epigenetically alleviates high-glucose-suppressed osteogenic differentiation of MC3T3-E1 cells. Eur Rev Med Pharmacol Sci. 2023 Aug;27(16):7576-7581.
[7] Hain BA, Jude B, Xu H, et al. Zoledronic Acid Improves Muscle Function in Healthy Mice Treated with Chemotherapy. J Bone Miner Res. 2020 Feb;35(2):368-381.
[8] Li W, Xu M, Shi X, et al. Effect of zoledronic acid on muscle metabolism in mice with osteoporosis combined with sarcopenia. BMC Musculoskelet Disord. 2024 Nov 21;25(1):937.
Zoledronic Acid是一种第三代含氮双膦酸盐类骨吸收抑制剂。Zoledronic Acid可通过抑制破骨细胞活性和诱导破骨细胞凋亡来减少骨钙释放和降低血钙水平。Zoledronic Acid通过抑制法尼基焦磷酸合成酶活性以阻断甲羟戊酸途径。Zoledronic Acid可用于骨质疏松症、Paget's病（变形性骨炎）、恶性肿瘤骨转移和恶性肿瘤引起的高钙血症的相关研究[1-4]。
在体外，Zoledronic Acid（0-300μM）处理CT26结肠癌细胞24-48h。Zoledronic Acid可抑制细胞增殖、诱导细胞凋亡并调节自噬[5]。在高葡萄糖条件下，Zoledronic Acid（1mM）处理MC3T3-E1细胞7天。Zoledronic Acid显著上调RUNX2、miR-133和miR-204的表达，同时下调MALAT1和miR-20a的表达[6]。
在体内，Zoledronic Acid（5μg/kg）每两天一次皮下注射，用于处理8周龄雌性Balb/c小鼠，持续10天。Zoledronic Acid防止了卡铂引起的骨丢失和肌肉无力[7]。Zoledronic Acid（100μg/kg）单次皮下注射于雄性C57BL/6J小鼠。Zoledronic Acid增加了体重和肌肉重量，改善了肌肉结构损伤，增加了I型肌纤维比例，并上调了β-catenin和AKT蛋白表达以及Wnt3a、Wnt16、Myf5和PI3K的mRNA表达[8]。
| Cell experiment [1]: | |
Cell lines | CT26 colon cancer cells |
Preparation Method | CT26 cells were cultured in DMEM medium supplemented with 10% fetal bovine serum in 5% CO₂ at 37°C. CT26 cells were treated with various concentrations of Zoledronic Acid (0-300μM) for 24 hours for viability and apoptosis assays. For Western blot analysis, cells were treated with 200μM Zoledronic Acid for 12h, 24h, 36h, and 48h. |
Reaction Conditions | 0-300μM; 12-48h |
Applications | Zoledronic Acid inhibited CT26 cell proliferation and induced apoptosis in a dose-dependent manner. Treatment with 200μM Zoledronic Acid for 36h and 48h significantly increased the expression of cleaved caspase-3 and p-p53. Treatment with 200μM Zoledronic Acid for 24h, 36h, and 48h significantly increased the expression of p62 and regulated the expression of beclin-1. |
| Animal experiment [2]: | |
Animal models | Female Balb/c mice |
Preparation Method | Mice were administered carboplatin (100mg/kg; i.p.) once, with or without Zoledronic Acid (5μg/kg; s.c.) every other day for 10 days. Mice were euthanized 10 days after injection. |
Dosage form | 5μg/kg; s.c.; every other day for 10 days |
Applications | Zoledronic Acid prevented carboplatin-induced bone loss in the distal femur and proximal tibia. Zoledronic Acid prevented carboplatin-induced muscle weakness (improved forelimb grip strength and EDL specific force to control levels), but did not prevent loss of body weight or muscle mass. |
References: | |
| Cas No. | 118072-93-8 | SDF | |
| 别名 | 唑来膦酸; Zoledronate; CGP 42446; CGP42446A; ZOL 446 | ||
| 化学名 | (1-hydroxy-2-imidazol-1-yl-1-phosphonoethyl)phosphonic acid | ||
| Canonical SMILES | C1=CN(C=N1)CC(O)(P(=O)(O)O)P(=O)(O)O | ||
| 分子式 | C5H10N2O7P2 | 分子量 | 272.09 |
| 溶解度 | ≥ 6.8mg/mL in Water with gentle warming | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.6753 mL | 18.3763 mL | 36.7525 mL |
| 5 mM | 735.1 μL | 3.6753 mL | 7.3505 mL |
| 10 mM | 367.5 μL | 1.8376 mL | 3.6753 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >99.00% Appearance: A solid
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