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165800-06-6

中文名稱 唑來磷酸一水化合物
英文名稱 Zoledronic acid hydrate
CAS 165800-06-6
分子式 C5H12N2O8P2
MDL 編號 MFCD08448695
分子量 290.1
MOL 文件 165800-06-6.mol
更新日期 2024/12/23 14:21:35
165800-06-6 結構式 165800-06-6 結構式

基本信息

中文別名
1-羥基-2-(咪唑-1-基)-亞乙基-1,1-二磷酸一水化物
唑來磷酸一水化合物
英文別名
[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
所屬類別
有機原料:雜環(huán)化合物

物理化學性質

熔點245 °C(dec.)
儲存條件2-8°C
溶解度H2O:≥2mg/mL
形態(tài)粉末
顏色白色至米色
Merck14,10187
InChIKeyFUXFIVRTGHOMSO-UHFFFAOYSA-N

安全數據

危險性符號(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險性描述H315-H319-H335
危險品標志Xi
危險類別碼36/37/38
安全說明26
WGK Germany3
RTECS號SZ8562450
海關編碼29332900
唑來磷酸一水化合物價格(試劑級)
報價日期產品編號產品名稱CAS號包裝價格
2024/11/11XW1658000662唑來磷酸一水化合物165800-06-65G544元
2024/11/11XW1658000661唑來磷酸一水化合物165800-06-61G146元
2024/11/0846621唑來磷酸
Zoledronic acid monohydrate
165800-06-61g853元

常見問題列表

生物活性
Zoledronic acid (Zoledronate, CGP-4244) monohydrate 是 Zoledronic acid (唑來膦酸) 的一水合物,是有效的破骨細胞抑制劑,可通過抑制甲戊二羥酸途徑的酶、阻止小GTP結合蛋白如Ras和Rho的異戊二烯化來誘導破骨細胞凋亡。
靶點
TargetValue
Ras
()
Rho
()
體外研究

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.
體內研究

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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