| Description | Tiludronate disodium (Tiludronic acid disodium) is an osteoclast vacuolar H(+)-ATPase inhibitor with antiresorptive and anti-inflammatory properties. Tiludronate disodium can be used in studies about metabolic bone disorders. |
| In vitro | Tiludronate displays potent inhibitory against proton transport in yeast microsomal preparations with an IC50 of 3.5 μM and inhibits the activity of purified yeast V-ATPase. Tiludronate inhibits proton transport with IC50s of 1.1 mM and 466 nM in kidney-derived vesicles and vesicles derived from osteoclasts[3]. |
| In vivo | Tiludronate dose-dependently inhibits the resorption of bones. Tiludronate reduces the secrete proton of mature osteoclasts into the resorption space and favors the detachment of mature osteoclasts from the bone matrix. Oral administration of Tiludronate (5-200 mg/kg) prevents the decrease in the skeletal mass in the castrated male rat model[3]. |
| Synonyms | Tiludronic Acid disodium, Tiludronic acid disodium |
| molecular weight | 362.57 |
| Molecular formula | C7H7ClNa2O6P2S |
| CAS | 149845-07-8 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | H2O: 56.2 mg/mL (155.1 mM), Sonication is recommended. |
| References | 1. Reginster JY, et al. Prevention of postmenopausal bone loss by tiludronate. Lancet. 1989 Dec 23-30;2(8678-8679):1469-71. 2. Nunes NLT, et al. Effects of local administration of tiludronic acid on experimental periodontitis in diabetic rats. J Periodontol. 2018 Jan;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. |