Introduction：Basic information about CAS 165800-07-7|Zoledronic Acid, Disodium Salt, Tetrahydrate, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | Zoledronic Acid, Disodium Salt, Tetrahydrate |
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| CAS Number | 165800-07-7 | Molecular Weight | 388.11400 |
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| Density | 2.13g/cm3 | Boiling Point | 764ºC at 760mmHg |
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| Molecular Formula | C5H16N2Na2O11P2 | Melting Point | 305-307ºC |
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| MSDS | / | Flash Point | 415.8ºC |
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Names
| Name | Zoledronic Acid, Disodium Salt, Tetrahydrate |
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| Synonym | More Synonyms |
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BiologicalActivity
| Description | Zoledronic Acid (Zoledronate) disodium tetrahydrate is a third-generation bisphosphonate (BP), with potent anti-resorptive activity. Zoledronic Acid disodium tetrahydrate inhibits the differentiation and apoptosis of osteoclasts. Zoledronic Acid disodium tetrahydrate also has anti-cancer effects[1]. |
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| Related Catalog | Signaling Pathways >>Apoptosis >>ApoptosisResearch Areas >>CancerSignaling Pathways >>Autophagy >>AutophagyResearch Areas >>Metabolic Disease |
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| In Vitro | Zoledronic Acid disodium tetrahydrate (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 disodium tetrahydrate increases the expression of osteoclastogenesis supporting factor from MLO-Y4 cells[2]. Zoledronic Acid disodium tetrahydrate enhances the RANKL expression via IL-6/ JAK2/STAT3 pathway in MLO-Y4 cells[2]. Zoledronic acid disodium tetrahydrate inhibits osteoclast differentiation and function through the regulation of NF-κB and JNK signalling pathways[3]. Zoledronic Acid disodium tetrahydrate (10-100 µM; 1-7 days) markedly reduces the viability of MC3T3-E1 cells and induces apoptosis in MC3T3-E1 cells[4]. Zoledronic Acid disodium tetrahydrate (10-100 µM; 4 days) inhibits cell viability due to the induction of apoptosis[4]. Zoledronic Acid disodium tetrahydrate exerts inhibitory effects on the differentiation and maturation of MC3T3-E1 cells at concentrations <1 µM[4]. 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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| In Vivo | Zoledronic Acid disodium tetrahydrate (0.05 mg/kg; i.p.; weekly; for 3 weeks) increases bone mineral density and content[5]. Zoledronic Acid disodium tetrahydrate (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]. 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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| References | [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. [6]. Shea GKH, et al. Oral Zoledronic acid bisphosphonate for the treatment of chronic low back pain with associated Modic changes: A pilot randomized controlled trial. J Orthop Res. 2022 Feb 23. |
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Chemical & Physical Properties
| Density | 2.13g/cm3 |
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| Boiling Point | 764ºC at 760mmHg |
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| Melting Point | 305-307ºC |
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| Molecular Formula | C5H16N2Na2O11P2 |
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| Molecular Weight | 388.11400 |
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| Flash Point | 415.8ºC |
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| Exact Mass | 388.00200 |
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| PSA | 215.31000 |
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| Vapour Pressure | 1.53E-24mmHg at 25°C |
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| InChIKey | IEJZOPBVBXAOBH-UHFFFAOYSA-L |
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| SMILES | O.O.O.O.O=P([O-])([O-])C(O)(Cn1ccnc1)P(=O)(O)O.[Na+].[Na+] |
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Safety Information
Customs
| HS Code | 2933290090 |
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| Summary | 2933290090. other compounds containing an unfused imidazole ring (whether or not hydrogenated) in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0% |
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Synonyms
| Sodium (1-hydroxy-2-(1H-imidazol-1-yl)-1-Phosphonoethyl)phosphonate tetrahydrate |
| Zoledronate disodium tetrahydrate |
