替鲁膦酸二钠半水合物 T39037

Product Introduction
Bioactivity


英文名: Tiludronate disodium hemihydrate

描述: Tiludronate (Tiludronic Acid) disodium hemihydrate is an orally active bisphosphonate compound that functions as an osteoregulator. It is primarily utilized in metabolic bone disorder research. This compound acts as a potent inhibitor of the osteoclast vacuolar H+ -ATPase and possesses antiresorptive and anti-inflammatory properties[4].

体外活性: The ability of Tiludronate to inhibit proton transport is 5-fold higher in kidney-derived vesicles (IC 50 =1.1 mM) and 10,000-fold higher in vesicles derived from osteoclasts (IC 50 =466 nM). Tiludronate also potently inhibited proton transport in yeast microsomal preparations (IC 50 =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].

体内活性: 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].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

关键字: Tiludronic acid | Tiludronate disodium hemihydrate | Tiludronate | Tiludronic acid disodium Hemihydrate | Tiludronate disodium Hemihydrate

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途