唑来磷酸一水化合物
- CAS号:165800-06-6
- 英文名:Zoledronic acid hydrate
- 中文名:唑来磷酸一水化合物
- CBNumber:CB5211391
- 分子式:C5H12N2O8P2
- 分子量:290.1
- MOL File:165800-06-6.mol
- 熔点 :245 °C(dec.)
- 储存条件 :2-8°C
- 溶解度 :H2O: ≥2mg/mL
- 形态 :powder
- 颜色 :white to beige
- Merck :14,10187
- InChIKey :FUXFIVRTGHOMSO-UHFFFAOYSA-N
- CAS 数据库 :165800-06-6(CAS DataBase Reference)
唑来磷酸一水化合物性质、用途与生产工艺
- 生物活性 Zoledronic acid (Zoledronate, CGP-4244) monohydrate 是 Zoledronic acid (唑来膦酸) 的一水合物，是有效的破骨细胞抑制剂，可通过抑制甲戊二羟酸途径的酶、阻止小GTP结合蛋白如Ras和Rho的异戊二烯化来诱导破骨细胞凋亡。
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靶点
Target Value Ras
()Rho
() -
体外研究
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. -
体内研究
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：2024/11/11
- 产品编号：XW1658000662
- 产品名称：唑来磷酸一水化合物
- CAS编号：165800-06-6
- 包装：5G
- 价格：544元
- 更新日期：2024/11/11
- 产品编号：XW1658000661
- 产品名称：唑来磷酸一水化合物
- CAS编号：165800-06-6
- 包装：1G
- 价格：146元
- 公司名称：Polpharma S.A.. Pharmaceutical Works
- 联系电话：--
- 电子邮件：dpo@polpharma.com
- 国家：波兰
- 产品数：18
- 优势度：58
- 公司名称：ZAKLADY FARMACEUTYCZNE POLPHARMA SA
- 联系电话：--
- 电子邮件：
- 国家：波兰
- 产品数：40
- 优势度：58
