Tiludronate disodium hemihydrate

Modify Date: 2024-01-13 19:39:06

Tiludronate disodium hemihydrate Structure
Tiludronate disodium hemihydrate structure
Common Name Tiludronate disodium hemihydrate
CAS Number 155453-10-4 Molecular Weight 743.15900
Density N/A Boiling Point N/A
Molecular Formula C14H16Cl2Na4O13P4S2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Tiludronate disodium hemihydrate


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

 Names

Name tetrasodium,[(4-chlorophenyl)sulfanyl-[hydroxy(oxido)phosphoryl]methyl]-hydroxyphosphinate,hydrate
Synonym More Synonyms

 Tiludronate disodium hemihydrate Biological Activity

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

[1]. Reginster JY, et al. Prevention of postmenopausal bone loss by tiludronate. Lancet. 1989;2(8678-8679):1469-1471.

[2]. Nunes NLT, et al. Effects of local administration of tiludronic acid on experimental periodontitis in diabetic rats. J Periodontol. 2018;89(1):105-116.

[3]. Bonjour JP, et al. Tiludronate: bone pharmacology and safety. Bone. 1995;17(5 Suppl):473S-477S.

[4]. David P, et al. The bisphosphonate tiludronate is a potent inhibitor of the osteoclast vacuolar H(+)-ATPase. J Bone Miner Res. 1996;11(10):1498-1507.

 Chemical & Physical Properties

Molecular Formula C14H16Cl2Na4O13P4S2
Molecular Weight 743.15900
Exact Mass 741.79500
PSA 340.51000
LogP 5.83070

 Synonyms

Phosphonic acid,(((4-chlorophenyl)thio)methylene)bis-,disodium salt,hydrate (2:1)
UNII-39SMX0W5WK
P,P'-(((4-Chlorophenyl)thio)methylene)bisphosphonic acid,disodium hemihydrate
Tiludronic acid disodium salt hemihydrate [MI]
Tiludronate disodium hemihydrate