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;唑来磷酸,一水合物;唑来磷酸一水合物, 骨吸收抑制剂;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);唑来磷酸一水化合物(CAS号:165800-06-6)

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;ZOLEDRONIC ACID MONOHYDRATE;ZoledronicacidforInjection;[1-hydroxy-2-(1H-imidazol-1-yl)ethane-1,1-diyl]bis(phosphonic acid) monohydrate

CAS号:

165800-06-6

分子式:

C5H12N2O8P2

分子量:

290.1

EINECS号:

相关类别:

医药原料;膦配体;有机磷;医药 高钙血;咪唑;抗肿瘤;原料药;Other APIs;Smad;TGF-beta;11;医用原料

Mol文件:

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)

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

Target Value Ras () Rho ()

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.

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.

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).

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.

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.

危险品标志 

Xi

危险类别码 

36/37/38

安全说明 

26

WGK Germany 

3

RTECS号

SZ8562450

海关编码 

29332900