1. Apoptosis
    Autophagy
  2. Apoptosis
    Autophagy
  3. Zoledronic acid monohydrate

Zoledronic acid monohydrate (Synonyms: Zoledronate monohydrate; CGP 42446 monohydrate; CGP42446A monohydrate; ZOL 446 monohydrate)

Cat. No.: HY-13777A Purity: ≥99.0%
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Zoledronic acid monohydrate (Zoledronate monohydrate) is a third-generation bisphosphonate (BP), with potent anti-resorptive activity. Zoledronic acid monohydrate inhibits the differentiation and apoptosis of osteoclasts. Zoledronic acid monohydrate also has anti-cancer effects.

For research use only. We do not sell to patients.

Zoledronic acid monohydrate Chemical Structure

Zoledronic acid monohydrate Chemical Structure

CAS No. : 165800-06-6

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Based on 1 publication(s) in Google Scholar

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Description

Zoledronic acid monohydrate (Zoledronate monohydrate) is a third-generation bisphosphonate (BP), with potent anti-resorptive activity. Zoledronic acid monohydrate inhibits the differentiation and apoptosis of osteoclasts. Zoledronic acid monohydrate also has anti-cancer effects[1].

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[2].
Zoledronic Acid monohydrate increases the expression of osteoclastogenesis supporting factor from MLO-Y4 cells[2].
Zoledronic Acid monohydrate enhances the RANKL expression via IL-6/ JAK2/STAT3 pathway in MLO-Y4 cells[2].
Zoledronic Acid monohydrate inhibits osteoclast differentiation and function through the regulation of NF-κB and JNK signalling pathways[3].
Zoledronic Acid monohydrate (10-100 µM; 1-7 days) markedly reduces the viability of MC3T3-E1 cells[4].
Zoledronic Acid monohydrate (10-100 µM; 1-7 days) induces apoptosis in MC3T3-E1 cells[4].
Zoledronic Acid monohydrate (10-100 µM; 4 days) inhibits cell viability due to the induction of apoptosis[4].
Zoledronic Acid monohydrate exerts inhibitory effects on the differentiation and maturation of MC3T3-E1 cells at concentrations <1 µM[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[4]

Cell Line: MC3T3-E1 cells
Concentration: 0.02 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[4]

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[4]

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.
In Vivo

Zoledronic Acid monohydrate (0.05 mg/kg; i.p.; weekly; for 3 weeks) increases bone mineral density and content[5].
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[5].

MCE 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.
Clinical Trial
Molecular Weight

290.10

Formula

C₅H₁₂N₂O₈P₂

CAS No.
SMILES

OC(P(O)(O)=O)(P(O)(O)=O)CN1C=CN=C1.[H]O[H]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

H2O : 14.29 mg/mL (49.26 mM; ultrasonic and adjust pH to 8 with NaOH)

H2O : 1 mg/mL (3.45 mM; Need ultrasonic)

DMSO : < 1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble or slightly soluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.4471 mL 17.2354 mL 34.4709 mL
5 mM 0.6894 mL 3.4471 mL 6.8942 mL
10 mM 0.3447 mL 1.7235 mL 3.4471 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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Keywords:

Zoledronic acidZoledronateCGP 42446CGP42446AZOL 446CGP42446CGP-42446ZOL446ZOL-446ApoptosisAutophagybisphosphonateanti-resorptiveosteoclastactivityosteoporosisanti-cancerInhibitorinhibitorinhibit

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Zoledronic acid monohydrate
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