Alendronate sodium trihydrate

Synonyms: G-704650, MK-217

Alendronate sodium trihydrate (G-704650, MK-217), a nitrogen-containing bisphosphonate, is a potent inhibitor of bone resorption used for the treatment and prevention of osteoporosis.

Alendronate sodium trihydrate Chemical Structure

Alendronate sodium trihydrate Chemical Structure

CAS: 121268-17-5

Selleck's Alendronate sodium trihydrate has been cited by 1 publication

Purity & Quality Control

Batch: Purity: 99.87%
99.87

Biological Activity

Description Alendronate sodium trihydrate (G-704650, MK-217), a nitrogen-containing bisphosphonate, is a potent inhibitor of bone resorption used for the treatment and prevention of osteoporosis.
In vitro
In vitro Alendronate, acting directly on osteoclasts, inhibits a rate-limiting step in the cholesterol biosynthesis pathway, essential for osteoclast function. [1] Alendronate inhibits the isoprenoid biosynthesis pathway and interferes with protein prenylation, as a result of reduced geranylgeranyl diphosphate levels. Alendronate inhibits the incorporation of [(3)H]mevalonolactone into proteins of 18-25 kDa and into nonsaponifiable lipids, including sterols in osteoclasts. [2] Alendronate causes a dose-dependent inhibition of [(3)H]MVA incorporation into sterols and a concomitant increase in incorporation of radiolabel into IPP and DMAPP. [3]
In Vivo
In vivo Alendronate causes erosions in the rabbit stomach, but not antral ulceration in rats. Alendronate increases the incidence and size of indomethacin-induced antral ulcers. Alendronate also enhances indomethacin-induced gastricdamage in the rat, and delayed gastric ulcer healing. [4] Alendronate (0.04-0.1 mg/kg twice weekly or 0.1 mg/kg weekly) partially blocks the establishment of bone metastases by human PC-3 ML cells and results in tumor formation in the peritoneum and other soft tissues. Alendronate pretreatment of mice (0.1 mg/kg twice weekly or weekly) and dosing along with taxol (10-50 mg/kg/day, twice weekly, or weekly) blocks the growth of PC-3 ML tumors in the bone marrow and soft tissues in a statistically significant manner and improves survival rates significantly by 4-5 weeks. [5]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05645289 Not yet recruiting Postmenopausal Osteoporosis Peking University Third Hospital January 1 2023 Phase 4
NCT03051620 Completed Osteoporosis Aarhus University Hospital|University of Aarhus February 1 2017 --
NCT02781805 Terminated Breast Neoplasms University of Wisconsin Madison|Wisconsin Partnership Program August 5 2016 Phase 1

Chemical lnformation & Solubility

Molecular Weight 326.13 Formula

C4H13NO7P2.3H2O.Na

CAS No. 121268-17-5 SDF Download Alendronate sodium trihydrate SDF
Smiles C(CC(O)(P(=O)(O)O)P(=O)(O)[O-])CN.O.O.O.[Na+]
Storage (From the date of receipt)

In vitro
Batch:

DMSO : Insoluble ( Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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