165800-06-6
165800-06-6 結(jié)構(gòu)式
基本信息
唑來(lái)磷酸一水化合物
(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
物理化學(xué)性質(zhì)
安全數(shù)據(jù)
制備方法
118072-93-8
165800-06-6
以(1-羥基-2-(1H-咪唑-1-基)乙烷-1,1-二基)二膦酸為原料合成1-羥基-2-(1-咪唑基)乙烷-1,1-二磷酸水合物的一般步驟如下： 實(shí)施例3：唑來(lái)膦酸一水合物的制備 將根據(jù)實(shí)施例1獲得的原始潮濕唑來(lái)膦酸（相當(dāng)于90.3g粗產(chǎn)物）懸浮于3050ml水中。在攪拌條件下，將懸浮液加熱至回流狀態(tài)。隨后，加入EPO水使總體積達(dá)到3750ml，直至完全溶解。停止加熱，繼續(xù)攪拌，使溶液緩慢冷卻至室溫。當(dāng)內(nèi)部溫度降至約70-80℃時(shí)，進(jìn)一步冷卻至2-5℃，并在此溫度下維持1小時(shí)。過(guò)濾沉淀，并用冰水洗滌。將所得沉淀置于氣流烘箱中干燥。最終，在5°C至60°C條件下獲得169.3g（產(chǎn)率89%）無(wú)色晶體。通過(guò)熱重分析（TGA）測(cè)得結(jié)晶水損失為6.8%，證實(shí)為一水合物。該物質(zhì)的X射線粉末衍射（XRPD）圖譜在2θ值為12.1°、12.8°、15.7°、18.9°±0.2°處顯示特征峰，與已知晶型I（US 2005/0054616）的衍射數(shù)據(jù)一致。圖1A展示了其XRPD圖譜，圖IV則展示了晶胞中原子的排列結(jié)構(gòu)。
參考文獻(xiàn)：
[1] Patent: WO2007/16982, 2007, A1. Location in patent: Page/Page column 7-8
[2] Patent: EP1925621, 2008, A1. Location in patent: Page/Page column 14
| 報(bào)價(jià)日期 | 產(chǎn)品編號(hào) | 產(chǎn)品名稱 | CAS號(hào) | 包裝 | 價(jià)格 |
| 2025/05/22 | 46621 | 唑來(lái)磷酸 Zoledronic acid monohydrate | 165800-06-6 | 1g | 682元 |
| 2025/05/22 | 46621 | 唑來(lái)磷酸 Zoledronic acid monohydrate | 165800-06-6 | 5g | 2267元 |
| 2025/05/22 | Z0031 | 唑來(lái)膦酸 一水合物 Zoledronic Acid Monohydrate | 165800-06-6 | 1g | 340元 |
常見問題列表
| Target | Value |
|
Ras
() | |
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Rho
() |
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. |
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. |