Etidronate

Catalog No.S1857

Etidronate  Chemical Structure

Molecular Weight(MW): 206.03

Etidronate is a non-aminobisphosphonate, show protein tyrosine phosphatase (PTP) inhibitory activity, used for the treatment of Paget's disease and the prevention of heterotopic ossification.

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Biological Activity

Description Etidronate is a non-aminobisphosphonate, show protein tyrosine phosphatase (PTP) inhibitory activity, used for the treatment of Paget's disease and the prevention of heterotopic ossification.
Targets
protein tyrosine phosphatase [6]
In vitro

Etidronate inhibits directly osteoclastic bone-resorbing activity by pit assay. Etidronate also directly induces apoptosis and disrupts actin rings in osteoclasts. [1]

In vivo Etidronate, when administered s.c. repeatedly at 10 or 40 mg/kg/day, gradually suppresses the adjuvant-induced allodynia In the rats with adjuvant arthritis, as assessed by 10-g von Frey hair. Etidronate (10-40 mg/kg/day) suppresses the adjuvant-induced mechanical allodynia in rat hindpaw. Etidronate (5–10 mg/kg/day) dose-dependently prevents the decrease in bone mineral density (BMD) in the proximal tibia of the arthritic rats. [2] Etidronate inhibits the histidine decarboxylase induction, but not the other inflammatory reactions induced by alendronate. Etidronate (unlike clodronate) also inhibits alendronate-induced BP-line formation in mice (even at 40 mmol/kg). Etidronate (160 mmol/kg) also inhibits the physicochemical changes in the tibia induced by six, weekly injections of alendronate. [3] Etidronate (10 mg/kg) combined with Calcitriol after subtotal nephrectomy (SNx) significantly inhibits thoracic and abdominal aortic calcification 3 weeks after the operation in rats. [4] Etidronate (5 mg/kg or 10 mg/kg) significantly reduces the thoracic and abdominal aortic calcification induced by calcitriol in the renal failure rat. Etidronate (5 mg/kg or 10 mg/kg) also reduces the dysfunction in aortic contraction. Etidronate (5 mg/kg) reverses the reduction in the aortic expression of matrix Gla protein mRNA observed in nephrectomized rats. [5]

Protocol

Solubility (25°C)

In vitro Water 41 mg/mL (199.0 mM)
DMSO Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 206.03
Formula

C2H8O7P2

CAS No. 2809-21-4
Storage powder
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01585402 Recruiting Arterial Calcification Due to CD73-Deficiency (ACDC) National Heart, Lung, and Blood Institute (NHLBI)|National Institutes of Health Clinical Center (CC) April 9, 2012 Phase 1
NCT01077817 Completed Esophageal Cancer|Squamous Cell Carcinoma|Adenocarcinoma Merck Sharp & Dohme Corp.|World Health Information Science Consultants, LLC February 2010 --
NCT00376662 Completed Osteoporosis British Thoracic Society August 1992 Phase 4

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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID