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

Cat. No.: HY-13777 Purity: 99.00%
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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.

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

Zoledronic Acid Chemical Structure

Zoledronic Acid Chemical Structure

CAS No. : 118072-93-8

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Customer Review

Based on 7 publication(s) in Google Scholar

Other Forms of Zoledronic Acid:

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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].

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].

MedChemExpress (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: 0.01 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 (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].

MedChemExpress (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

272.09

Formula

C5H10N2O7P2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OC(P(O)(O)=O)(P(O)(O)=O)CN1C=CN=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

H2O : 4.81 mg/mL (17.68 mM; ultrasonic and warming and adjust pH to 6 with NaOH and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.6753 mL 18.3763 mL 36.7525 mL
5 mM 0.7351 mL 3.6753 mL 7.3505 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 8.7 mg/mL (31.97 mM); Clear solution; Need ultrasonic and adjust pH to 8 with 1M NaOH

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: 99.00%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O 1 mM 3.6753 mL 18.3763 mL 36.7525 mL 91.8814 mL
5 mM 0.7351 mL 3.6753 mL 7.3505 mL 18.3763 mL
10 mM 0.3675 mL 1.8376 mL 3.6753 mL 9.1881 mL
15 mM 0.2450 mL 1.2251 mL 2.4502 mL 6.1254 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Zoledronic Acid Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Zoledronic Acid
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