Tiludronate disodium hemihydrate
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| 包装规格: | 100mg in glass bottle |
| 产品描述: | 基本信息 产品编号: T11140 产品名称: Tiludronate disodium hemihydrate CAS: 155453-10-4 储存条件 粉末 -20℃ 四年 分子式: C7H9ClO6P2S.1/2H2O.2Na 溶于液体 -80℃ 一年 分子量: 371.57 化学名: tetrasodium;[(4-chlorophenyl)sulfanyl-[hydroxy(oxido)phosphoryl]methyl]-hydroxyphosphinate;hydrate Solubility (25°C): 体外: DMSO Ethanol Water 体内(现配现用): <1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 生物活性 产品描述 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 disodium hemihydrate是破骨细胞空泡H+-ATP酶的有效抑制剂。 靶点 Proton Pump 体外研究 The ability of Tiludronate to inhibit proton transport is 5-fold higher in kidney-derived vesicles (IC50=1.1mM) and 10,000-fold higher in vesicles derived from osteoclasts (IC50=466nM).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. 体内研究 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 (5-200mg/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. |
| 保存条件: | -20℃ |
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