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

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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) 纯度: ≥98.0%

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。

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

Zoledronic acid monohydrate Chemical Structure

CAS No. : 165800-06-6

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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[1].

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[2].
Zoledronic Acid monohydrate increases the expression of osteoclastogenesis supporting factor from MLO-Y4 cells[2].
Zoledronic Acid monohydrate enhances the RANKL expression via IL-6/ JAK2/STAT3 pathway in MLO-Y4 cells[2].
Zoledronic Acid monohydrate inhibits osteoclast differentiation and function through the regulation of NF-κB and JNK signalling pathways[3].
Zoledronic Acid monohydrate (10-100 µM; 1-7 days) markedly reduces the viability of MC3T3-E1 cells[4].
Zoledronic Acid monohydrate (10-100 µM; 1-7 days) induces apoptosis in MC3T3-E1 cells[4].
Zoledronic Acid monohydrate (10-100 µM; 4 days) inhibits cell viability due to the induction of apoptosis[4].
Zoledronic Acid monohydrate exerts inhibitory effects on the differentiation and maturation of MC3T3-E1 cells at concentrations <1 µm[4].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[4]

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[4]

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[4]

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
(In Vivo)

Zoledronic Acid monohydrate (0.05 mg/kg; i.p.; weekly; for 3 weeks) increases bone mineral density and content[5].
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[5].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Five-week-old C57BL6 mice[5]
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.

Clinical Trial

分子量

290.10

Formula

C5H12N2O8P2

CAS 号

165800-06-6

中文名称

唑来膦酸一水合物

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
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
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)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.4471 mL 17.2354 mL 34.4709 mL
5 mM 0.6894 mL 3.4471 mL 6.8942 mL
10 mM 0.3447 mL 1.7235 mL 3.4471 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

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.

    [3]. Xiao-Lin Huang, et al. Zoledronic acid inhibits osteoclast differentiation and function through the regulation of NF-κB and JNK signalling pathways. Int J Mol Med. 2019 Aug;44(2):582-592.

    [4]. XIN HUANG, et al. Dose-dependent inhibitory effects of zoledronic acid on osteoblast viability and function in vitro. Mol Med Rep. 2016 Jan; 13(1): 613-622.

    [5]. Samantha Pozzi, et al. High-dose zoledronic acid impacts bone remodeling with effects on osteoblastic lineage and bone mechanical properties. Clin Cancer Res. 2009 Sep 15;15(18):5829-39.

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