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

Name: Zoledronic acid monohydrate
Brand: MedChemExpress
SKU: HY-13777A
Rating: 5.0 (12 reviews)

Cat. No.: HY-13777A Purity: 99.88%: FAQs
Data Sheet SDS COA Handling Instructions Technical Support

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.

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Zoledronic acid monohydrate Chemical Structure

CAS No. : 165800-06-6

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50 mg	In-stock	Estimated Time of Arrival: December 31
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Based on 12 publication(s) in Google Scholar

Other Forms of Zoledronic acid monohydrate:

Zoledronic Acid Get quote
Zoledronic acid disodium tetrahydrate Get quote
Zoledronic acid (monohydrate) (Standard) Get quote

12 Publications Citing Use of MCE Zoledronic acid monohydrate

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Biological Activity
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References
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Description

Cellular Effect

Cell Line	Type	Value	Description	References
BXPC-3	IC₅₀	10 μM Compound: Zoledronate	Cytotoxicity against human BXPC-3 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay Cytotoxicity against human BXPC-3 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 33132173]
CFPAC-1	IC₅₀	10 μM Compound: Zoledronate	Cytotoxicity against human CFPAC-1 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay Cytotoxicity against human CFPAC-1 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 33132173]
Erythrocyte	IC₅₀	> 200 μM Compound: NBP3	Antiparasitic activity against Plasmodium falciparum 3D7 infected in human erythrocyte assessed as intraerythrocytic growth inhibition incubated for 24 hrs followed by [3H]hypoxanthine addition by microbeta scintillation counter analysis Antiparasitic activity against Plasmodium falciparum 3D7 infected in human erythrocyte assessed as intraerythrocytic growth inhibition incubated for 24 hrs followed by [3H]hypoxanthine addition by microbeta scintillation counter analysis	[PMID: 33522236]
HCT-116	IC₅₀	61.582 μM Compound: ZOL	Cytotoxicity against FPPS-positive human HCT116 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay Cytotoxicity against FPPS-positive human HCT116 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay	[PMID: 31785819]
HL-60	IC₅₀	595.8 μM Compound: Zoledronic acid	Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay	[PMID: 24928399]
Huh-7	IC₅₀	60 μM Compound: Zoledronate	Cytotoxicity against human HuH7 cells after 144 hrs by MTT assay Cytotoxicity against human HuH7 cells after 144 hrs by MTT assay	[PMID: 24607589]
JJN-3	EC₅₀	9.4 μM Compound: 1	Antiproliferative activity against human JJN-3 after 72 hrs by MTT assay Antiproliferative activity against human JJN-3 after 72 hrs by MTT assay	[PMID: 22390415]
K562	EC₅₀	> 100 μM Compound: Zoledronate	Activation of butyrophilin 3A1 in human K562 cells assessed as interferon-gamma production pretreated for 15 mins followed by HMBPP-treated Vgamma9Vdelta2 T cells addition and measured after 20 hrs by ELISA Activation of butyrophilin 3A1 in human K562 cells assessed as interferon-gamma production pretreated for 15 mins followed by HMBPP-treated Vgamma9Vdelta2 T cells addition and measured after 20 hrs by ELISA	[PMID: 31531198]
K562	EC₅₀	23 μM Compound: Zoledronate	Activation of butyrophilin 3A1 in human K562 cells assessed as interferon-gamma production pretreated for 240 mins followed by HMBPP-treated Vgamma9Vdelta2 T cells addition and measured after 20 hrs by ELISA Activation of butyrophilin 3A1 in human K562 cells assessed as interferon-gamma production pretreated for 240 mins followed by HMBPP-treated Vgamma9Vdelta2 T cells addition and measured after 20 hrs by ELISA	[PMID: 31531198]
K562	EC₅₀	79 μM Compound: Zoledronate	Activation of butyrophilin 3A1 in human K562 cells assessed as interferon-gamma production pretreated for 60 mins followed by HMBPP-treated Vgamma9Vdelta2 T cells addition and measured after 20 hrs by ELISA Activation of butyrophilin 3A1 in human K562 cells assessed as interferon-gamma production pretreated for 60 mins followed by HMBPP-treated Vgamma9Vdelta2 T cells addition and measured after 20 hrs by ELISA	[PMID: 31531198]
LoVo	IC₅₀	34.914 μM Compound: ZOL	Cytotoxicity against FPPS-positive human Lovo cells assessed as reduction in cell viability measured after 48 hrs by MTT assay Cytotoxicity against FPPS-positive human Lovo cells assessed as reduction in cell viability measured after 48 hrs by MTT assay	[PMID: 31785819]
MCF7	IC₅₀	23 μM Compound: Zoledronic acid	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 24928399]
MCF7	IC₅₀	27.7 μM Compound: 2	Antiproliferative activity against human MCF7 cell line by MTT assay Antiproliferative activity against human MCF7 cell line by MTT assay	[PMID: 16970405]
MDA-MB-231	IC₅₀	> 100 μM Compound: ZOL	Cytotoxicity against FPPS-negative human MDA-MB-231 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay Cytotoxicity against FPPS-negative human MDA-MB-231 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay	[PMID: 31785819]
MIA PaCa-2	EC₅₀	13.4 μM Compound: 6	Cytotoxicity against human MIAPaCa2 cells assessed as decrease in cell growth measured after 72 hrs by MTT assay Cytotoxicity against human MIAPaCa2 cells assessed as decrease in cell growth measured after 72 hrs by MTT assay	[PMID: 31725297]
NCI-H460	IC₅₀	11.7 μM Compound: 2	Antiproliferative activity against human NCI-H460 cell line by MTT assay Antiproliferative activity against human NCI-H460 cell line by MTT assay	[PMID: 16970405]
PANC-1	IC₅₀	10 μM Compound: Zoledronate	Cytotoxicity against human PANC-1 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay Cytotoxicity against human PANC-1 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 33132173]
PANC-1	EC₅₀	16.1 μM Compound: 6	Cytotoxicity against human PANC1 cells assessed as decrease in cell growth measured after 72 hrs by MTT assay Cytotoxicity against human PANC1 cells assessed as decrease in cell growth measured after 72 hrs by MTT assay	[PMID: 31725297]
RPMI-8226	EC₅₀	11 μM Compound: 1; ZOL	Antiproliferative activity against human RPMI8226 cells after 72 hrs by MTT assay Antiproliferative activity against human RPMI8226 cells after 72 hrs by MTT assay	[PMID: 30016091]
RPMI-8226	EC₅₀	11 μM Compound: 1	Cytotoxicity against human RPMI8226 cells after 72 hrs by MTT assay Cytotoxicity against human RPMI8226 cells after 72 hrs by MTT assay	[PMID: 23998921]
SF-268	IC₅₀	14.3 μM Compound: 2	Antiproliferative activity against human SF-268 cell line by MTT assay Antiproliferative activity against human SF-268 cell line by MTT assay	[PMID: 16970405]
T-cell	IC₅₀	170 μM Compound: 1	Activation of human CD4+ Vgamma2/Vdelta2 T cell clone JN.23 assessed as TNF-alpha release after 16 hrs by sandwich ELISA in presence of antigen presenting cell line, CP.EBV Activation of human CD4+ Vgamma2/Vdelta2 T cell clone JN.23 assessed as TNF-alpha release after 16 hrs by sandwich ELISA in presence of antigen presenting cell line, CP.EBV	[PMID: 23610597]

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].

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:	0.02 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].

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

290.10

Formula

C₅H₁₂N₂O₈P₂

CAS No.

165800-06-6

Appearance

Solid

Color

White to off-white

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)

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

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. 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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: 3.33 mg/mL (11.48 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

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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: 99.88%

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Data Sheet (287 KB) SDS (393 KB)

COA (259 KB) RP-HPLC (258 KB)

Handling Instructions (2659 KB)

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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O	1 mM	3.4471 mL	17.2354 mL	34.4709 mL	86.1772 mL
	5 mM	0.6894 mL	3.4471 mL	6.8942 mL	17.2354 mL
	10 mM	0.3447 mL	1.7235 mL	3.4471 mL	8.6177 mL
	15 mM	0.2298 mL	1.1490 mL	2.2981 mL	5.7451 mL
	20 mM	0.1724 mL	0.8618 mL	1.7235 mL	4.3089 mL
	25 mM	0.1379 mL	0.6894 mL	1.3788 mL	3.4471 mL
	30 mM	0.1149 mL	0.5745 mL	1.1490 mL	2.8726 mL
	40 mM	0.0862 mL	0.4309 mL	0.8618 mL	2.1544 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.

Zoledronic acid monohydrate Related Classifications

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

Customer Review

Other Forms of Zoledronic acid monohydrate:

12 Publications Citing Use of MCE Zoledronic acid monohydrate

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

Customer Review

Other Forms of Zoledronic acid monohydrate:

Zoledronic acid monohydrate Related Antibodies

12 Publications Citing Use of MCE Zoledronic acid monohydrate

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Purity & Documentation

References

Customer Review

Zoledronic acid monohydrate Related Antibodies

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Complete Stock Solution Preparation Table

Zoledronic acid monohydrate Related Classifications

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