唑来磷酸一水化合物

生物活性靶点体外研究体内研究唑来磷酸一水化合物试剂级价格

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

唑来磷酸一水化合物化学性质

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)

安全信息

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

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。
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.