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Tiludronate

CAS No. : 89987-06-4

MCE 国际站：Tiludronate

产品活性：Tiludronate (Tiludronic Acid) 是一种口服活性双膦酸盐，可以起到骨调节作用。Tiludronate用于代谢性骨疾病的研究。Tiludronate 是破骨细胞空泡 H(+)-ATP 酶的有效抑制剂。

研究领域：Membrane Transporter/Ion Channel

作用靶点：Proton Pump

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.

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.

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