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165800-06-6

中文名称 唑来磷酸一水化合物
英文名称 Zoledronic acid hydrate
CAS 165800-06-6
分子式 C5H12N2O8P2
MDL 编号 MFCD08448695
分子量 290.1
MOL 文件 165800-06-6.mol
更新日期 2024/04/25 08:39:42
165800-06-6 结构式 165800-06-6 结构式

基本信息

中文别名
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
英文别名
[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
ZOLEDRONIC ACID MONOHYDRATE
ZoledronicacidforInjection
所属类别
有机原料:杂环化合物

物理化学性质

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
Merck14,10187
InChIKeyFUXFIVRTGHOMSO-UHFFFAOYSA-N

安全数据

危险性符号(GHS)
GHS07
警示词警告
危险性描述H315-H319-H335
危险品标志Xi
危险类别码36/37/38
安全说明26
WGK Germany3
RTECS号SZ8562450
海关编码29332900
唑来磷酸一水化合物价格(试剂级)
报价日期产品编号产品名称CAS号包装价格
2024/01/25HY-13777A唑来磷酸一水化合物
Zoledronic acid monohydrate
165800-06-650mg800元
2024/01/25HY-13777A唑来磷酸一水化合物
Zoledronic acid monohydrate
165800-06-6100mg1548元
2024/01/16Z0031唑来膦酸 一水合物
Zoledronic Acid Monohydrate
165800-06-61g290元

常见问题列表

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。
靶点
TargetValue
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.
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