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Zoledronic Acid (Synonyms: 唑来膦酸; Zoledronate; CGP 42446; CGP42446A; ZOL 446)
Zoledronic Acid (Zoledronate) 是第三代含氮二磷酸盐，具有高效的抗骨质再吸收活性。Zoledronic Acid 能抑制破骨细胞的分化和凋亡。Zoledronic Acid 也有抗癌作用。
Zoledronic Acid Chemical Structure
CAS No. : 118072-93-8
| 规格 |
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是否有货 |
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| 100 mg |
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询价 |
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| 250 mg |
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询价 |
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| 500 mg |
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Zoledronic Acid 的其他形式现货产品:
Zoledronic acid monohydrate
| 生物活性 |
Zoledronic Acid (Zoledronate) is a third-generation bisphosphonate (BP), with potent anti-resorptive activity. Zoledronic Acid inhibits the differentiation and apoptosis of osteoclasts. Zoledronic Acid also has anti-cancer effects[1].
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体外研究
(In Vitro) |
Zoledronic Acid (0.1-1 µM; 48 hours) increases receptor activator of nuclear factor kB ligand (RANKL) and sclerostin mRNA expressions in osteocyte-like MLO-Y4 cells[2].
Zoledronic Acid increases the expression of osteoclastogenesis supporting factor from MLO-Y4 cells[2].
Zoledronic Acid enhances the RANKL expression via IL-6/ JAK2/STAT3 pathway in MLO-Y4 cells[2].
Zoledronic acid inhibits osteoclast differentiation and function through the regulation of NF-κB and JNK signalling pathways[3].
Zoledronic Acid (10-100 µM; 1-7 days) markedly reduces the viability of MC3T3-E1 cells[4].
Zoledronic Acid (10-100 µM; 1-7 days) induces apoptosis in MC3T3-E1 cells[4].
Zoledronic Acid (10-100 µM; 4 days) inhibits cell viability due to the induction of apoptosis[4].
Zoledronic Acid exerts inhibitory effects on the differentiation and maturation of MC3T3-E1 cells at concentrations <1 µm[4].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay[4]
| Cell Line: |
MC3T3-E1 cells |
| Concentration: |
0.01 µM , 0.1 µM, 1 µM, 10 µM, 100 µM |
| Incubation Time: |
1 day, 3 days, 5 days, 7 days |
| Result: |
Reduced cells viability at 10 µM and 100 µM. |
Apoptosis Analysis[4]
| Cell Line: |
MC3T3-E1 cells |
| Concentration: |
0.01 µM , 0.1 µM, 1 µM, 10 µM, 100 µM |
| Incubation Time: |
1 days, 4 days, 7 days |
| Result: |
Increased the number of early apoptotic cells and late apoptotic or necrotic cells at dose-dependent and time-dependent (high concentrations). |
Western Blot Analysis[4]
| Cell Line: |
MC3T3-E1 cells |
| Concentration: |
0.01 µM , 0.1 µM, 1 µM, 10 µM, 100 µM |
| Incubation Time: |
4 days |
| Result: |
Down-regulated the protein level of inactive caspase-3 and up-regulated the protein level of active caspase-3 at the concentrations of 10 and 100 µM. |
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体内研究
(In Vivo) |
Zoledronic Acid (0.05 mg/kg; i.p.; weekly; for 3 weeks) increases bone mineral density and content[5].
Zoledronic Acid (0.5-1 mg/kg; i.p.; weekly; for 3 weeks) inhibits both osteoclast and osteoblasts function and bone remodeling in vivo interfering with bone mechanical properties[5].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: |
Five-week-old C57BL6 mice[5] |
| Dosage: |
0.05 mg/kg, 0.5 mg/kg, 1 mg/kg |
| Administration: |
Intraperitoneal injection, weekly, for 3 weeks |
| Result: |
Inhibited both osteoclast and osteoblasts function and bone remodeling at 0.5 mg/kg and 1 mg/kg. |
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis.
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| 参考文献 |
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[1]. Lianwei Wang, et al. Various pathways of zoledronic acid against osteoclasts and bone cancer metastasis: a brief review. BMC Cancer. 2020; 20: 1059.
[2]. Hyung Joon Kim, et al. Zoledronate Enhances Osteocyte-Mediated Osteoclast Differentiation by IL-6/RANKL Axis. Int J Mol Sci. 2019 Mar; 20(6): 1467.
[3]. Xiao-Lin Huang, et al. Zoledronic acid inhibits osteoclast differentiation and function through the regulation of NF-κB and JNK signalling pathways. Int J Mol Med. 2019 Aug;44(2):582-592.
[4]. XIN HUANG, et al. Dose-dependent inhibitory effects of zoledronic acid on osteoblast viability and function in vitro. Mol Med Rep. 2016 Jan; 13(1): 613-622.
[5]. Samantha Pozzi, et al. High-dose zoledronic acid impacts bone remodeling with effects on osteoblastic lineage and bone mechanical properties. Clin Cancer Res. 2009 Sep 15;15(18):5829-39.
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