唑来磷酸一水化合物
| 中文名称 | 唑来磷酸一水化合物 |
|---|---|
| 中文同义词 | 1-羟基-2-(咪唑-1-基)-亚乙基-1,1-二磷酸一水化物;唑来磷酸一水化合物;唑来膦酸单水合物;唑来磷酸(标准品);唑来磷酸一水化合物(唑来膦酸一水化合物、唑仑膦酸一水化合物);唑来磷酸,一水合物;唑来磷酸一水化合物(CAS号:165800-06-6);唑来磷酸一水合物, 骨吸收抑制剂 |
| 英文名称 | Zoledronic acid hydrate |
| 英文同义词 | [1-HYDROXY-(1H-IMIDAZOL-1-YL)-PHOSPHONOETHYL] PHOSPHONIC ACID MONOHYDRATE;(1-hydroxy-2-imidazol-1-yl-1-phosphono-ethyl)phosphonic acid hydrate;(1-hydroxy-2-imidazol-1-ylethylidene)diphosphonic acid monohydrate;PHOSPHONIC ACID, [1-HYDROXY-2-(1H-IMIDAZOL-1-YL)ETHYLIDENE]BIS-, MONOHYDRATE;zoledronic acid hydrate;ZoledronicacidforInjection;[1-hydroxy-2-(1H-imidazol-1-yl)ethane-1,1-diyl]bis(phosphonic acid) monohydrate;P,P′-[1-Hydroxy-2-(1H-imidazol-1-yl)ethylidene]bisphosphonic acid monohydrate |
| CAS号 | 165800-06-6 |
| 分子式 | C5H12N2O8P2 |
| 分子量 | 290.1 |
| EINECS号 | |
| 相关类别 | 膦配体;有机磷;咪唑;抗肿瘤;原料药;Other APIs;Smad;TGF-beta;医药 高钙血;11;医药原料;医用原料 |
| Mol文件 | 165800-06-6.mol |
| 结构式 |  |
唑来磷酸一水化合物 性质
| 熔点 | 245 °C(dec.) |
|---|---|
| 储存条件 | 2-8°C |
| 溶解度 | H2O：≥2mg/mL |
| 形态 | 粉末 |
| 颜色 | 白色至米色 |
| Merck | 14,10187 |
| InChIKey | FUXFIVRTGHOMSO-UHFFFAOYSA-N |
| CAS 数据库 | 165800-06-6(CAS DataBase Reference) |
| Target | Value |
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Ras
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Rho
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Zoledronic Acid monohydrate (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 monohydrate increases the expression of osteoclastogenesis supporting factor from MLO-Y4 cells.
Zoledronic Acid monohydrate enhances the RANKL expression via IL-6/ JAK2/STAT3 pathway in MLO-Y4 cells.
Zoledronic Acid monohydrate inhibits osteoclast differentiation and function through the regulation of NF-κB and JNK signalling pathways.
Zoledronic Acid monohydrate (10-100 µM; 1-7 days) markedly reduces the viability of MC3T3-E1 cells.
Zoledronic Acid monohydrate (10-100 µM; 1-7 days) induces apoptosis in MC3T3-E1 cells.
Zoledronic Acid monohydrate (10-100 µM; 4 days) inhibits cell viability due to the induction of apoptosis.
Zoledronic Acid monohydrate exerts inhibitory effects on the differentiation and maturation of MC3T3-E1 cells at concentrations <1 µM.
Cell Viability Assay
| Cell Line: | MC3T3-E1 cells |
| Concentration: | 0.02 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
| Cell Line: | MC3T3-E1 cells |
| Concentration: | 0.02 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
| Cell Line: | MC3T3-E1 cells |
| Concentration: | 0.02 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 monohydrate (0.05 mg/kg; i.p.; weekly; for 3 weeks) increases bone mineral density and content.
Zoledronic Acid monohydrate (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. |
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/01/25 | HY-13777A | 唑来磷酸一水化合物 Zoledronic acid monohydrate | 165800-06-6 | 50mg | 800元 |
| 2024/01/25 | HY-13777A | 唑来磷酸一水化合物 Zoledronic acid monohydrate | 165800-06-6 | 100mg | 1548元 |