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

Cat. No.: HY-13777 Purity: 99.94%
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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.

CAS No. : 118072-93-8

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Based on 24 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Zoledronic Acid purchased from MedChemExpress. Usage Cited in: JCI Insight. 2025 Jan 30:e184468.  [Abstract]

    Serum creatinine, urea nitrogen, and uric acid levels in CKD mice or sham-operated mice (Zoledronic Acid: i.p., 20/100 μg/kg, once per day, 4 weeks).

    Zoledronic Acid purchased from MedChemExpress. Usage Cited in: Commun Biol. 2024 Nov 9;7(1):1476.  [Abstract]

    Representative images and statistical graph of transwell assays from the indicated groups after treatment with ZOL at different concentrations (0, 10 and 20 μM) in UM-UC-3 cells and T24 cells for 48 h.

    Zoledronic Acid purchased from MedChemExpress. Usage Cited in: Commun Biol. 2024 Nov 9;7(1):1476.  [Abstract]

    An MTT assay was performed to detect changes in the proliferation of BLCA cells (UM-UC-3, T24 and 5637) after treatment with different concentrations (0, 1, 2, 5, 10, 20, 40, 60 and 80 μM) of ZOL for 48 h.

    Zoledronic Acid purchased from MedChemExpress. Usage Cited in: Commun Biol. 2024 Nov 9;7(1):1476.  [Abstract]

    Western blot analyses of EMT-related proteins in ZOL-treated ((0, 10 and 20 μM, 48 h) UM-UC-3, T24 and 5637 cells. GAPDH was used as the loading control.

    Zoledronic Acid purchased from MedChemExpress. Usage Cited in: Commun Biol. 2024 Nov 9;7(1):1476.  [Abstract]

    ZOL (100 μg/kg, intraperitoneally injection, three times a week for 4 weeks). Representative images of H&E-stained mouse lung tissue sections (n = 3)and statistical analysis of the number of metastatic nodules in H&E-stained mouse lung tissue sections.

    Zoledronic Acid purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Mar 21;15(1):2529.  [Abstract]

    Representative TRAP staining images of femur cortical bone and quantification of TRAP positive cell number from PBS or zoledronic acid (100 µg/kg, intraperitoneal injection, once per week for 2 weeks) treated 4-week-old Dmp1Cre-DTAki/wt mice.

    Zoledronic Acid purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Mar 21;15(1):2529.  [Abstract]

    Representative confocal images of femur cortical bone and quantitative result of TCVs from PBS or zoledronic acid (100 µg/kg, intraperitoneal injection, once per week for 2 weeks) treated 4-week-old Dmp1Cre-DTAki/wt mice.
    • 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].

    Cellular Effect
    Cell Line Type Value Description References
    PBMC EC50
    18500 nM
    Compound: 2, Zol
    Induction of Vgamma9Vdelta2 T cell activation in human PBMC cells assessed as CD69+ CD25+ cells incubated for 12 hrs by flow cytometric analysis
    Induction of Vgamma9Vdelta2 T cell activation in human PBMC cells assessed as CD69+ CD25+ cells incubated for 12 hrs by flow cytometric analysis
    [PMID: 39026632]
    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 : 4.17 mg/mL (15.33 mM; ultrasonic and warming 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
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    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: 99.94%

    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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    • 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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    Product Name:
    Zoledronic Acid
    Cat. No.:
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