Zoledronic Acid, Disodium Salt, Tetrahydrate

Modify Date: 2024-01-09 20:48:56

Zoledronic Acid, Disodium Salt, Tetrahydrate Structure
Zoledronic Acid, Disodium Salt, Tetrahydrate structure
Common Name Zoledronic Acid, Disodium Salt, Tetrahydrate
CAS Number 165800-07-7 Molecular Weight 388.11400
Density 2.13g/cm3 Boiling Point 764ºC at 760mmHg
Molecular Formula C5H16N2Na2O11P2 Melting Point 305-307ºC
MSDS N/A Flash Point 415.8ºC

 Use of Zoledronic Acid, Disodium Salt, Tetrahydrate


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].

 Names

Name Zoledronic Acid, Disodium Salt, Tetrahydrate
Synonym More Synonyms

  Biological Activity

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].
Related Catalog
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.
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.
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.

 Chemical & Physical Properties

Density 2.13g/cm3
Boiling Point 764ºC at 760mmHg
Melting Point 305-307ºC
Molecular Formula C5H16N2Na2O11P2
Molecular Weight 388.11400
Flash Point 415.8ºC
Exact Mass 388.00200
PSA 215.31000
Vapour Pressure 1.53E-24mmHg at 25°C

 Safety Information

HS Code 2933290090

 Customs

HS Code 2933290090
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%

 Synonyms

Sodium (1-hydroxy-2-(1H-imidazol-1-yl)-1-Phosphonoethyl)phosphonate tetrahydrate
Zoledronate disodium tetrahydrate