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编 号：F199133
分子式：C5H18N2Na2O11P2
分子量：390.13
分子式：C5H18N2Na2O11P2
分子量：390.13
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CAS No: 165800-07-7
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生物活性：
Zoledronic Acid (Zoledronate) disodium tetrahydrate is a third-generation bisphosphonate (BP), with potent anti-resorptive activity. Zoledronic Acid disodium tetrahydrate inhibits the differentiation and apoptosis of osteoclasts. Zoledronic Acid disodium tetrahydrate also has anti-cancer effects.
体内研究：
Zoledronic Acid disodium tetrahydrate (0.05 mg/kg; i.p.; weekly; for 3 weeks) increases bone mineral density and content.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.Animal Model:Five-week-old C57BL6 mice
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.
体外研究：
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.Zoledronic Acid disodium tetrahydrate increases the expression of osteoclastogenesis supporting factor from MLO-Y4 cells.Zoledronic Acid disodium tetrahydrate enhances the RANKL expression via IL-6/ JAK2/STAT3 pathway in MLO-Y4 cells.Zoledronic acid disodium tetrahydrate inhibits osteoclast differentiation and function through the regulation of NF-κB and JNK signalling pathways.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.Zoledronic Acid disodium tetrahydrate (10-100 μM; 4 days) inhibits cell viability due to the induction of apoptosis.Zoledronic Acid disodium tetrahydrate exerts inhibitory effects on the differentiation and maturation of MC3T3-E1 cells at concentrations Zoledronic acid disodium tetrahydrate 相关抗体:Cell Viability AssayCell 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 AnalysisCell 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 AnalysisCell 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.
Zoledronic Acid (Zoledronate) disodium tetrahydrate is a third-generation bisphosphonate (BP), with potent anti-resorptive activity. Zoledronic Acid disodium tetrahydrate inhibits the differentiation and apoptosis of osteoclasts. Zoledronic Acid disodium tetrahydrate also has anti-cancer effects.
体内研究：
Zoledronic Acid disodium tetrahydrate (0.05 mg/kg; i.p.; weekly; for 3 weeks) increases bone mineral density and content.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.Animal Model:Five-week-old C57BL6 mice
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.
体外研究：
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.Zoledronic Acid disodium tetrahydrate increases the expression of osteoclastogenesis supporting factor from MLO-Y4 cells.Zoledronic Acid disodium tetrahydrate enhances the RANKL expression via IL-6/ JAK2/STAT3 pathway in MLO-Y4 cells.Zoledronic acid disodium tetrahydrate inhibits osteoclast differentiation and function through the regulation of NF-κB and JNK signalling pathways.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.Zoledronic Acid disodium tetrahydrate (10-100 μM; 4 days) inhibits cell viability due to the induction of apoptosis.Zoledronic Acid disodium tetrahydrate exerts inhibitory effects on the differentiation and maturation of MC3T3-E1 cells at concentrations Zoledronic acid disodium tetrahydrate 相关抗体:Cell Viability AssayCell 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 AnalysisCell 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 AnalysisCell 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.
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