Zoledronic acid monohydrate|165800-06-6|(唑来膦酸一水合物; Zoledronate monohydrate; CGP 42446 monohydrate; CGP42446A monohydrate; ZOL 446 monohydrate)-陌孚医药/Medlife

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Zoledronic acid monohydrate (Synonyms: 唑来膦酸一水合物; Zoledronate monohydrate; CGP 42446 monohydrate; CGP42446A monohydrate; ZOL 446 monohydrate)

目录号: PL11801 纯度: ≥98.0%

CAS No. :165800-06-6

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中文名称	Zoledronic acid monohydrate
中文别名	唑来磷酸一水化合物;1-羟基-2-(咪唑-1-基)-亚乙基-1,1-二磷酸一水化物唑来膦酸单水合物;唑来膦酸单水合物;Zoledronic Acid Monohydrate 唑来膦酸单水合物;他克莫司;唑来磷酸;唑来磷酸一水;唑来磷酸一水合物;唑来膦酸;唑来膦酸一水合物;1-羟基-2-(1-咪唑基)乙烷-1,1-二磷酸;1-羟基-2-(咪唑-1-基)-亚乙基-1,1-二磷酸一水化物;1-羟基-2-(1-咪唑基)乙烷-1,1-二磷酸一水合物;唑来磷酸(标准品);唑来磷酸一水合物, 骨吸收抑制剂;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,一水合物
英文名称	Zoledronic acid monohydrate
英文别名	Zoledronic acid hydrate;(1-Hydroxy-2-imidazol-1-yl-1-phosphono-ethyl)phosphonic acid hydrate;(1-Hydroxy-2-imidazol-1-ylethylidene)diphosphonic acid monohydrate;Zoledronic Acid Monohydrate;(1-Hydroxy-2-(1H-imidazol-1-yl)ethane-1,1-diyl)diphosphonic acid hydrate;Zoledronic Acid;Zoledronic Acid (hydrate);(1-hydroxy-2-imidazol-1-yl-1-phosphonoethyl)phosphonic acid,hydrate;1-Hydroxy-2-(1-imidazolyl)ethane-1,1-diphosphonic Acid Monohydrate;CGP 42446 monohydrate;CGP42446A monohydrate;ZOL 446 monohydrate;Zoledronate monohydrate;P,P′-[1-Hydroxy-2-(1H-imidazol-1-yl)ethylidene]bisphosphonic acid monohydrate;[1-hydroxy-2-(1H-imidazol-1-yl)ethane-1,1-diyl]bis(phosphonic acid) monohydrate;Acid, the;oledronic acid;ZoledronicacidforInjection;Zoledronic acid (CGP 42446) monohydrate;1-Hydroxy-2-(1-imidazolyl)ethane-1,1-diphos;Zoledronic acid monohydrate;zoledronic acid hydrate;ZOLEDRONIC ACID MONOHYDRATE;Zoledronic acid monohydrate, >=99%;Zoledronic acid monohydrate, 98%, Bone resorption inhibitor
Cas No.	165800-06-6
分子式	C₅H₁₂N₂O₈P₂
分子量	290.10
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

Zoledronic Acid monohydrate (Zoledronate monohydrate) 是第三代含氮二磷酸盐，具有高效的抗骨质再吸收活性。Zoledronic Acid monohydrate 能抑制破骨细胞的分化和凋亡。Zoledronic Acid monohydrate 也有抗癌作用。

生物活性

Zoledronic acid monohydrate (Zoledronate monohydrate) is a third-generation bisphosphonate (BP), with potent anti-resorptive activity. Zoledronic acid monohydrate inhibits the differentiation and apoptosis of osteoclasts. Zoledronic acid monohydrate also has anti-cancer effects.

性状

Solid

体外研究(In Vitro)

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

体内研究(In Vivo)

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.
has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[1]. Lianwei Wang, et al. Various pathways of zoledronic acid against osteoclasts and bone cancer metastasis: a brief review. BMC Cancer. 2020; 20: 1059.
[2]. Hyung Joon Kim, et al. Zoledronate Enhances Osteocyte-Mediated Osteoclast Differentiation by IL-6/RANKL Axis. Int J Mol Sci. 2019 Mar; 20(6): 1467.

溶解度数据	In Vitro: H₂O : 14.29 mg/mL (49.26 mM; ultrasonic and adjust pH to 8 with NaOH)DMSO : < 1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble or slightly soluble)

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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