化合物 Zoledronic acid disodium tetrahydrate T61764

Product Introduction
Bioactivity


英文名: Zoledronic acid disodium tetrahydrate

描述: Zoledronic Acid (Zoledronate) disodium tetrahydrate is a potent third-generation bisphosphonate (BP), exhibiting strong anti-resorptive activity. It effectively inhibits osteoclast differentiation and apoptosis, while also demonstrating anti-cancer properties [1].

体外活性: Zoledronic Acid disodium tetrahydrate (0.1-1 μM; 48 hours) increases receptor activator of nuclear factor kB ligand (RANKL) and sclerostin mRNA expressions in osteocyte-like MLO-Y4 cells [2]. Zoledronic Acid disodium tetrahydrate increases the expression of osteoclastogenesis supporting factor from MLO-Y4 cells [2]. Zoledronic Acid disodium tetrahydrate enhances the RANKL expression via IL-6/ JAK2/STAT3 pathway in MLO-Y4 cells [2]. Zoledronic acid disodium tetrahydrate inhibits osteoclast differentiation and function through the regulation of NF-κB and JNK signalling pathways [3]. Zoledronic Acid disodium tetrahydrate (10-100 μM; 1-7 days) markedly reduces the viability of MC3T3-E1 cells and induces apoptosis in MC3T3-E1 cells [4]. Zoledronic Acid disodium tetrahydrate (10-100 μM; 4 days) inhibits cell viability due to the induction of apoptosis [4]. Zoledronic Acid disodium tetrahydrate exerts inhibitory effects on the differentiation and maturation of MC3T3-E1 cells at concentrations <1 μM [4]. Cell Viability Assay [4] Cell Line: MC3T3-E1 cells Concentration: 0.01 μM, 0.1 μM, 1 μM, 10 μM, 100 μM Incubation Time: 1 day, 3 days, 5 days, 7 days Result: Reduced cells viability at 10 μM and 100 μM. Apoptosis Analysis [4] Cell Line: MC3T3-E1 cells Concentration: 0.01 μM, 0.1 μM, 1 μM, 10 μM, 100 μM Incubation Time: 1 days, 4 days, 7 days Result: Increased the number of early apoptotic cells and late apoptotic or necrotic cells at dose-dependent and time-dependent (high concentrations). Western Blot Analysis [4] Cell Line: MC3T3-E1 cells Concentration: 0.01 μM, 0.1 μM, 1 μM, 10 μM, 100 μM Incubation Time: 4 days Result: Down-regulated the protein level of inactive caspase-3 and up-regulated the protein level of active caspase-3 at the concentrations of 10 and 100 μM.

体内活性: Zoledronic Acid disodium tetrahydrate (0.05 mg/kg; i.p.; weekly; for 3 weeks) increases bone mineral density and content [5]. Zoledronic Acid disodium tetrahydrate (0.5-1 mg/kg; i.p.; weekly; for 3 weeks) inhibits both osteoclast and osteoblasts function and bone remodeling in vivo interfering with bone mechanical properties [5]. Animal Model: Five-week-old C57BL6 mice [5] Dosage: 0.05 mg/kg, 0.5 mg/kg, 1 mg/kg Administration: Intraperitoneal injection, weekly, for 3 weeks Result: Inhibited both osteoclast and osteoblasts function and bone remodeling at 0.5 mg/kg and 1 mg/kg.

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

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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