Zoledronic Acid (Zoledronate; CGP 42446)

Alias: CGP42446; CGP42446A; ZOL446; CGP-42446; CGP-42446A; ZOL-446; CGP 42446; CGP 42446A; ZOL 446; Zoledronate, trade names: Zometa; Reclast

Cat No.:V1560 Purity: ≥98%

COA Product Data Instructions for use SDS

Zoledronic acid (Zoledronate; CGP-42446; CGP42446A; ZOL-446; Zometa; Reclast) is potent bisphosphonate with anti-bone-resorption activity.

Zoledronic Acid (Zoledronate; CGP 42446) Chemical Structure CAS No.: 118072-93-8
Product category: Rho

This product is for research use only, not for human use. We do not sell to patients.

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Other Forms of Zoledronic Acid (Zoledronate; CGP 42446):

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Top Publications Citing lnvivochem Products

Nature 2021, 597(7874):119-125.

Cell 2020,183:1202-1218.e25.

Science Adv 2022: 8, eabm9427.

Nature 597, 119–125 (2021)

Cell Stem Cell 2020,26(6):845-861.e12.

Science Trans Med 2023,15(701):eadd7872.

STTT 2023,8(1):91.

Cell Reports 2023,42(4):112313

Science Trans Med 2023, 15: eadd7872.

Cancer Cell 2021,39(4):529-547.e7.

Cancer Discov 2022,12(4):1106-1127.

Immunity 2023,56(3):620-634.e11.

J Am Chem Soc 2022,144:21831-21836.

Cell 2020,183:1202-1218.e25.

Science Adv 2022:8,eabm9427.

Nature 2021,597(7874):119-125.

Cell 2020,183:1202-1218.e25.

PNAS Nexus 2022,1(3):pgac063.

ACS Nano 2023,17(10):9110-9125.

Biomaterial 2023 Sep16:302:122333.

Purity & Quality Control Documentation

Current batch：

Purity: ≥98%

COA

MSDS

NMR

Instructions

Product Description
Bioactivity & Protocols
Physicochemical Properties
Solubility Data
Calculators
Biological Data

Product Description

Zoledronic acid (Zoledronate; CGP-42446; CGP42446A; ZOL-446; Zometa; Reclast) is potent bisphosphonate with anti-bone-resorption activity. The mevalonate pathway enzymes are inhibited, and small GTP-binding proteins like Rho and Ras are not isoprenylated, causing osteoclasts to undergo apoptosis. Approved for the treatment of osteoporosis, cancer-related elevated blood calcium, cancer-related bone loss, Paget's disease of the bone, and Duchenne muscular dystrophy, zoledronic acid is a type of medication. A synthetic analog of pyrophosphate with imidazole bisphosphonate and anti-bone-resorption properties is zoledronic acid. By binding to hydroxyapatite crystals in the bone matrix, zoledronic acid, a bisphosphonate of the third generation, inhibits the formation and aggregation of these crystals as well as their quick dissolution.

Biological Activity I Assay Protocols (From Reference)

Targets

Rho; Ras

ln Vitro

Zoledronic Acid (0.1-1 µM; 48 hours) increases the expression of sclerostin and receptor activator of nuclear factor kB ligand (RANKL) mRNA in osteocyte-like MLO-Y4 cells[2].
Zoledronic Acid increases the expression of osteoclastogenesis supporting factor in MLO-Y4 cells[2].
Zoledronic acid increases the expression of RANKL in MLO-Y4 cells through the IL-6/JAK2/STAT3 pathway[2].
Zoledronic acid suppresses osteoclast function and differentiation by controlling the JNK and NF-κB signaling pathways[3].
MC3T3-E1 cells' viability is significantly decreased by zoledronic acid (10–100 µM; 1–7 days)[4].
Zoledronic Acid (10-100 µM; 1-7 days) induces apoptosis in MC3T3-E1 cells[4].
Zoledronic Acid (10-100 µM; 4 days) induces apoptosis, which inhibits cell viability[4].
Zoledronic Acid, at concentrations less than 1 µM, inhibits the differentiation and maturation of MC3T3-E1 cells[4].

ln Vivo

Zoledronic Acid (0.05 mg/kg; i.p.; weekly; for 3 weeks) increases bone mineral in terms of content and density[5].
Zoledronic Acid (0.5–1 mg/kg; intraperitoneal; weekly; for three weeks) interferes with the mechanical properties of bone by inhibiting the function of osteoblasts and osteoclasts as well as bone remodeling in vivo[5].

Cell Assay

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.

Animal Protocol

Five-week-old C57BL6 mice 0.05 mg/kg, 0.5 mg/kg, 1 mg/kg Intraperitoneal injection, weekly, for 3 weeks

References

[1]. Various pathways of zoledronic acid against osteoclasts and bone cancer metastasis: a brief review. BMC Cancer. 2020; 20: 1059.

[2]. Zoledronate Enhances Osteocyte-Mediated Osteoclast Differentiation by IL-6/RANKL Axis. Int J Mol Sci. 2019 Mar; 20(6): 1467.

[3]. 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.

[4]. Dose-dependent inhibitory effects of zoledronic acid on osteoblast viability and function in vitro. Mol Med Rep. 2016 Jan; 13(1): 613-622.

[5]. 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.

[6]. 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.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Physicochemical Properties

Molecular Formula	C5H10N2O7P2
Molecular Weight	272.09
Exact Mass	271.99632466
CAS #	118072-93-8
Related CAS #	Zoledronic acid monohydrate;165800-06-6;Zoledronic acid disodium tetrahydrate;165800-07-7
Appearance	Solid
SMILES	C1=CN(C=N1)CC(O)(P(=O)(O)O)P(=O)(O)O
InChi Key	XRASPMIURGNCCH-UHFFFAOYSA-N
InChi Code	InChI=1S/C5H10N2O7P2/c8-5(15(9,10)11,16(12,13)14)3-7-2-1-6-4-7/h1-2,4,8H,3H2,(H2,9,10,11)(H2,12,13,14)
Chemical Name	(1-hydroxy-2-imidazol-1-yl-1-phosphonoethyl)phosphonic acid
Synonyms	CGP42446; CGP42446A; ZOL446; CGP-42446; CGP-42446A; ZOL-446; CGP 42446; CGP 42446A; ZOL 446; Zoledronate, trade names: Zometa; Reclast
Storage	Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Solubility Data

Solubility (In Vitro)

DMSO: < 1 mg/mL

Water: < 1 mg/mL (neutral pH); 10-15mg/mL (pH = 8)

Ethanol: < 1 mg/mL

Solubility (In Vivo)

30% PEG400+0.5% Tween80+5%Propylene glycol: 10 mg/mL

(Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		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
	10 mM	0.3675 mL	1.8376 mL	3.6753 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Mass

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Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

Calculate the Mass of a compound required to prepare a solution of known volume and concentration
Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?

Enter 350.26 in the Molecular Weight (MW) box
Enter 10 in the Concentration box and choose the correct unit (mM)
Enter 5 in the Volume box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

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Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:

Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
Enter 25 into the Concentration (End) box and select the correct unit (mM)
Enter 25 into the Volume (End) box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box

Molecular formula

Total molecular weight

g/mol

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Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4 c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
Click the “Calculate” button
The answer appears in the Volume (to add to vial) box

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)

Dosage mg/kg

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Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)

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Calculation results

Working concentration： mg/mL；

Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O，mix and clarify.

Note： (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.

Biological Data

ZA inhibits the RANKL/RANK pathway. BMC Cancer . 2020 Nov 3;20(1):1059.
ZA inhibits mevalonate pathway. BMC Cancer . 2020 Nov 3;20(1):1059.
ZA induces caspase-dependent apoptosis, reverts chemoresistance and stimulats immune response in cancer cells through Ras/Erk1/2 pathway. BMC Cancer . 2020 Nov 3;20(1):1059.