1. Metabolic Enzyme/Protease
  2. Phosphatase
  3. Neridronate

Neridronate is an aminobisphosphonate. Neridronate induces osteoblast differentiation, enhances alkaline phosphatase activity and mineralized nodule formation. Neridronate inhibits endothelial cell proliferation, fibroblast growth factor-2-induced capillary-like tube formation, and angiogenesis. Neridronate can be used for osteogenesis imperfecta and Paget’s disease of bone.

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

Neridronate

Neridronate Chemical Structure

CAS No. : 79778-41-9

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Based on 1 publication(s) in Google Scholar

Other Forms of Neridronate:

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  • Biological Activity

  • Purity & Documentation

  • References

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Description

Neridronate is an aminobisphosphonate. Neridronate induces osteoblast differentiation, enhances alkaline phosphatase activity and mineralized nodule formation. Neridronate inhibits endothelial cell proliferation, fibroblast growth factor-2-induced capillary-like tube formation, and angiogenesis. Neridronate can be used for osteogenesis imperfecta and Paget’s disease of bone[1][2][3].

Cellular Effect
Cell Line Type Value Description References
HFF IC50
59.7 μM
Compound: 34
In vitro inhibitory concentration against the growth of Toxoplasma gondii in human foreskin fibroblast monolayer cells (HFF cells)
In vitro inhibitory concentration against the growth of Toxoplasma gondii in human foreskin fibroblast monolayer cells (HFF cells)
[PMID: 15857119]
T-cell IC50
1.96 μM
Compound: 45
Inhibitory activity, for stimulation of TNF-alpha release in gamma-delta T cells, using individual observed maximum TNF-alpha release
Inhibitory activity, for stimulation of TNF-alpha release in gamma-delta T cells, using individual observed maximum TNF-alpha release
[PMID: 14711309]
T-cell IC50
503 μM
Compound: 45
Inhibitory activity, for stimulation of TNF-alpha release in gamma-delta T cells, using a constrained maximum TNF-alpha release of 2700 pg/mL
Inhibitory activity, for stimulation of TNF-alpha release in gamma-delta T cells, using a constrained maximum TNF-alpha release of 2700 pg/mL
[PMID: 14711309]
Vero IC50
> 200 μM
Compound: 10
Inhibition of Trypanosoma cruzi Amastigotes was determined in Vero cells culture and fetal calf serum
Inhibition of Trypanosoma cruzi Amastigotes was determined in Vero cells culture and fetal calf serum
[PMID: 11300872]
In Vitro

Neridronate (≤10-8-10-3 M; 0-20 days) at 10-3 M causes cytotoxicity and cell death in primary human osteoblasts grown in 10% FCS over 20 days, 10-4 M inhibits proliferation, 10-5 to 10-7 M increases viable cell counts, and concentrations ≤10-8 M have no effect on viability or proliferation[1].
Neridronate (10-7-10-4 M; 4-8 days) at 10-5 to 10-7 M increases type I collagen synthesis in primary human osteoblasts grown in 10% FCS after 4 days, while 10-4 to 10-6 M reduces synthesis after 8 days[1].
Neridronate (10-8-10-7 M; 10-20 days) at 10-8 M maximally increases ALKP activity by 50% in primary human osteoblasts grown in 10% FCS after 10 days, and 10-7 M increases activity by 22% after 20 days[1].
Neridronate (10-8-10-4 M; 4-20 days) at 10-4 M increases mineralized nodule formation in primary human osteoblasts grown in 2% UG after 4 days, while 10-7 and 10-8 M increase formation by 44% and 24%, respectively, after 20 days[1].
Neridronate (1-50 μM; 24 h) dose-dependently inhibits the proliferation of human umbilical vein endothelial cells, with peak activity at 30 μM after 24 h of treatment[2].
Neridronate (30 μM; 18 h) disrupts FGF-2-induced capillary-like tube formation by human umbilical vein endothelial cells seeded on Matrigel after 18 h of incubation[2].

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

Cell Proliferation Assay[2]

Cell Line: human umbilical vein endothelial cells (HUVECs)
Concentration: 1 μM, 3 μM, 10 μM, 30 μM, 50 μM
Incubation Time: 24 h
Result: Reduced HUVEC growth in a dose-dependent fashion, with peak inhibition at 30 μM; 50 μM produced a plateau effect.
Showed statistically significant inhibition at 10 μM, 30 μM, and 50 μM.
In Vivo

Neridronate (50 μM/embryo; via gelatin sponge on CAM; single administration on day 8 of incubation) significantly reduces FGF-2-induced angiogenesis in the chick embryo CAM assay[2].

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

Animal Model: White Leghorn (fertilized eggs)[2]
Dosage: 50 μM/embryo
Administration: via gelatin sponge on CAM; single administration on day 8 of incubation
Result: Reduced the mean number of FGF-2-induced blood vessels entering the sponge to 15 ± 3 (compared to 30 ± 4 for FGF-2 alone).
Clinical Trial
Molecular Weight

277.15

Formula

C6H17NO7P2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OC(P(O)(O)=O)(CCCCCN)P(O)(O)=O

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 : 5 mg/mL (18.04 mM; ultrasonic and warming and adjust pH to 8 with NaOH and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.6082 mL 18.0408 mL 36.0815 mL
5 mM 0.7216 mL 3.6082 mL 7.2163 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)

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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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C2

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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: 2 mg/mL (7.22 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

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: 98.0%

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. 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 3.6082 mL 18.0408 mL 36.0815 mL 90.2039 mL
5 mM 0.7216 mL 3.6082 mL 7.2163 mL 18.0408 mL
10 mM 0.3608 mL 1.8041 mL 3.6082 mL 9.0204 mL
15 mM 0.2405 mL 1.2027 mL 2.4054 mL 6.0136 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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Neridronate
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