1. Tiludronate

Tiludronate (Tiludronic Acid), an orally active bisphosphonate, can act an osteoregulator. Tiludronate is used for the research of the metabolic bone disorders. Tiludronate is a potent inhibitor of the osteoclast vacuolar H(+)-ATPase. Antiresorptive and anti-inflammatory properties.

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Tiludronate Chemical Structure

Tiludronate Chemical Structure

CAS No. : 89987-06-4

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Description

Tiludronate (Tiludronic Acid), an orally active bisphosphonate, can act an osteoregulator. Tiludronate is used for the research of the metabolic bone disorders. Tiludronate is a potent inhibitor of the osteoclast vacuolar H(+)-ATPase. Antiresorptive and anti-inflammatory properties[1][2][3][4].

In Vitro

The ability of Tiludronate to inhibit proton transport is 5-fold higher in kidney-derived vesicles (IC50=1.1 mM) and 10,000-fold higher in vesicles derived from osteoclasts (IC50=466 nM). Tiludronate also potently inhibited proton transport in yeast microsomal preparations (IC50=3.5 microM) and inhibited the activity of purified yeast V-ATPase. The inhibition of the osteoclast V-ATPase-mediated proton transport by Tiludronate is rapid, pH-dependent, and reversible[3].

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

In Vivo

Tiludronate exerts a dose-dependent inhibitory activity on bone resorption. Tiludronate could act on mature osteoclasts by reducing their capacity to secrete proton into the resorption space and also by favoring their detachment from the bone matrix. Tiludronate is also tested in other models of osteoporosis. In the castrated male rat model, Tiludronate (5-200 mg/kg; p.o.) prevents the decrease in the skeletal mass, assessed physically by measuring the bone weight and density or chemically by determining the calcium and phosphate content[3].

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

Clinical Trial
Molecular Weight

318.61

Formula

C7H9ClO6P2S

CAS No.
SMILES

O=P(O)(O)C(P(O)(O)=O)SC1=CC=C(Cl)C=C1

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    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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Tiludronate
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HY-A0213
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