Zoledronic acid monohydrate

SKU: orb1940453

Description

Zoledronic acid hydrate is a synthetic imidazole bisphosphonate analog with anti-bone-resorption activity.

Images & Validation

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Key Properties

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CAS Number	165800-06-6
MW	290.105
Purity	>98% (HPLC)
Formula	C₅H₁₂N₂O₈P₂
SMILES	O.OC(Cn1ccnc1)(P(O)(O)=O)P(O)(O)=O
Target	Apoptosis
Solubility	In Vitro: H2O : 14.29 mg/mL (49.26 mM)

Bioactivity

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In Vivo

Zoledronic Acid monohydrate (0.05 mg/kg; i.p.; weekly; for 3 weeks) increases bone mineral density and content. Zoledronic Acid monohydrate (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. Animal model: Five-week-old C57BL6 mice. 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.

In Vitro

Zoledronic Acid monohydrate (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. Zoledronic Acid monohydrate increases the expression of osteoclastogenesis supporting factor from MLO-Y4 cells. Zoledronic Acid monohydrate enhances the RANKL expression via IL-6/ JAK2/STAT3 pathway in MLO-Y4 cells. Zoledronic Acid monohydrate inhibits osteoclast differentiation and function through the regulation of NF-κB and JNK signalling pathways. Zoledronic Acid monohydrate (10-100 μM; 1-7 days) markedly reduces the viability of MC3T3-E1 cells. Zoledronic Acid monohydrate (10-100 μM; 1-7 days) induces apoptosis in MC3T3-E1 cells. Zoledronic Acid monohydrate (10-100 μM; 4 days) inhibits cell viability due to the induction of apoptosis. Zoledronic Acid monohydrate exerts inhibitory effects on the differentiation and maturation of MC3T3-E1 cells at concentrations <1 μM. Cell Viability Assay Cell line: MC3T3-E1 cells. Concentration: 0.02 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 Cell line: MC3T3-E1 cells. Concentration: 0.02 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. Cell line: MC3T3-E1 cells. Concentration: 0.02 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.

Storage & Handling

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Storage	Storage temperature: -20°C. Stability: ≥ 2 years
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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Gene Symbol

Apoptosis

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