Home Metabolism phosphatase inhibitor Etidronate

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Etidronate phosphatase inhibitor

Cat.No.S1857

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

Chemical Structure

Molecular Weight: 206.03

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S185701 Water]41 mg/mL]false]DMSO]Insoluble]false]Ethanol]Insoluble]false Purity: 99.17%
99.17

Chemical Information, Storage & Stability

Molecular Weight 206.03 Formula

C2H8O7P2

 Storage (From the date of receipt)
CAS No. 2809-21-4 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CC(O)(P(=O)(O)O)P(=O)(O)O

Solubility

In vitro
Batch:

Water : 41 mg/mL

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

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

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.

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Mechanism of Action

Targets/IC50/Ki
protein tyrosine phosphatase [6]
In vitro
Etidronate inhibits directly osteoclastic bone-resorbing activity by pit assay. This compound 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. This compound (10-40 mg/kg/day) suppresses the adjuvant-induced mechanical allodynia in rat hindpaw. It (5–10 mg/kg/day) dose-dependently prevents the decrease in bone mineral density (BMD) in the proximal tibia of the arthritic rats. [2] This chemical inhibits the histidine decarboxylase induction, but not the other inflammatory reactions induced by alendronate. It (unlike clodronate) also inhibits alendronate-induced BP-line formation in mice (even at 40 mmol/kg). This compound (160 mmol/kg) also inhibits the physicochemical changes in the tibia induced by six, weekly injections of alendronate. [3] It (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] This chemical (5 mg/kg or 10 mg/kg) significantly reduces the thoracic and abdominal aortic calcification induced by calcitriol in the renal failure rat. It (5 mg/kg or 10 mg/kg) also reduces the dysfunction in aortic contraction. This compound (5 mg/kg) reverses the reduction in the aortic expression of matrix Gla protein mRNA observed in nephrectomized rats. [5]
References
  • https://pubmed.ncbi.nlm.nih.gov/16141638/
  • https://pubmed.ncbi.nlm.nih.gov/17270170/
  • https://pubmed.ncbi.nlm.nih.gov/19199933/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02673060 Completed
Bone Metastasis
Osteros Biomedica Ltd
 July 2014 Phase 1
NCT01585402 Completed
Arterial Calcification|CD73 Deficiency
National Heart Lung and Blood Institute (NHLBI)|National Institutes of Health Clinical Center (CC)
 August 20 2012 Phase 2

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