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Tiludronate

CAS No. : 89987-06-4

MCE 國際站：Tiludronate

產品活性：Tiludronate (Tiludronic Acid) 是一種口服活性雙膦酸鹽，可以起到骨調節作用。Tiludronate用于代謝性骨疾病的研究。Tiludronate 是破骨細胞空泡 H(+)-ATP 酶的有效抑制劑。

研究領域：Membrane Transporter/Ion Channel

作用靶點：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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熱門產品線：重組蛋白? |? 藥物篩選? |? 天然產物? |? 熒光染料? |? PROTAC? |? 同位素標記物

Trending products：Recombinant Proteins? |? Bioactive Screening Libraries? |? Natural Products? |? Dye Reagents? |? PROTAC? |? Isotope-Labeled Compounds

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