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: HY-13777A 纯度: 99.88%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

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。

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Zoledronic acid monohydrate Chemical Structure

CAS No. : 165800-06-6

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50 mg	￥800	In-stock
100 mg	￥1548	In-stock
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Other Forms of Zoledronic acid monohydrate:

Zoledronic Acid In-stock
Zoledronic acid disodium tetrahydrate 询价
Zoledronic acid monohydrate (Standard) 询价

MCE 顾客使用本产品发表的 12 篇科研文献

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生物活性
纯度 & 产品资料
参考文献

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].

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
BXPC-3	IC₅₀	10 μM Compound: Zoledronate	Cytotoxicity against human BXPC-3 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay Cytotoxicity against human BXPC-3 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 33132173]
CFPAC-1	IC₅₀	10 μM Compound: Zoledronate	Cytotoxicity against human CFPAC-1 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay Cytotoxicity against human CFPAC-1 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 33132173]
Erythrocyte	IC₅₀	> 200 μM Compound: NBP3	Antiparasitic activity against Plasmodium falciparum 3D7 infected in human erythrocyte assessed as intraerythrocytic growth inhibition incubated for 24 hrs followed by [3H]hypoxanthine addition by microbeta scintillation counter analysis Antiparasitic activity against Plasmodium falciparum 3D7 infected in human erythrocyte assessed as intraerythrocytic growth inhibition incubated for 24 hrs followed by [3H]hypoxanthine addition by microbeta scintillation counter analysis	[PMID: 33522236]
HCT-116	IC₅₀	61.582 μM Compound: ZOL	Cytotoxicity against FPPS-positive human HCT116 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay Cytotoxicity against FPPS-positive human HCT116 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay	[PMID: 31785819]
HL-60	IC₅₀	595.8 μM Compound: Zoledronic acid	Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay	[PMID: 24928399]
Huh-7	IC₅₀	60 μM Compound: Zoledronate	Cytotoxicity against human HuH7 cells after 144 hrs by MTT assay Cytotoxicity against human HuH7 cells after 144 hrs by MTT assay	[PMID: 24607589]
JJN-3	EC₅₀	9.4 μM Compound: 1	Antiproliferative activity against human JJN-3 after 72 hrs by MTT assay Antiproliferative activity against human JJN-3 after 72 hrs by MTT assay	[PMID: 22390415]
K562	EC₅₀	> 100 μM Compound: Zoledronate	Activation of butyrophilin 3A1 in human K562 cells assessed as interferon-gamma production pretreated for 15 mins followed by HMBPP-treated Vgamma9Vdelta2 T cells addition and measured after 20 hrs by ELISA Activation of butyrophilin 3A1 in human K562 cells assessed as interferon-gamma production pretreated for 15 mins followed by HMBPP-treated Vgamma9Vdelta2 T cells addition and measured after 20 hrs by ELISA	[PMID: 31531198]
K562	EC₅₀	23 μM Compound: Zoledronate	Activation of butyrophilin 3A1 in human K562 cells assessed as interferon-gamma production pretreated for 240 mins followed by HMBPP-treated Vgamma9Vdelta2 T cells addition and measured after 20 hrs by ELISA Activation of butyrophilin 3A1 in human K562 cells assessed as interferon-gamma production pretreated for 240 mins followed by HMBPP-treated Vgamma9Vdelta2 T cells addition and measured after 20 hrs by ELISA	[PMID: 31531198]
K562	EC₅₀	79 μM Compound: Zoledronate	Activation of butyrophilin 3A1 in human K562 cells assessed as interferon-gamma production pretreated for 60 mins followed by HMBPP-treated Vgamma9Vdelta2 T cells addition and measured after 20 hrs by ELISA Activation of butyrophilin 3A1 in human K562 cells assessed as interferon-gamma production pretreated for 60 mins followed by HMBPP-treated Vgamma9Vdelta2 T cells addition and measured after 20 hrs by ELISA	[PMID: 31531198]
LoVo	IC₅₀	34.914 μM Compound: ZOL	Cytotoxicity against FPPS-positive human Lovo cells assessed as reduction in cell viability measured after 48 hrs by MTT assay Cytotoxicity against FPPS-positive human Lovo cells assessed as reduction in cell viability measured after 48 hrs by MTT assay	[PMID: 31785819]
MCF7	IC₅₀	23 μM Compound: Zoledronic acid	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 24928399]
MCF7	IC₅₀	27.7 μM Compound: 2	Antiproliferative activity against human MCF7 cell line by MTT assay Antiproliferative activity against human MCF7 cell line by MTT assay	[PMID: 16970405]
MDA-MB-231	IC₅₀	> 100 μM Compound: ZOL	Cytotoxicity against FPPS-negative human MDA-MB-231 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay Cytotoxicity against FPPS-negative human MDA-MB-231 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay	[PMID: 31785819]
MIA PaCa-2	EC₅₀	13.4 μM Compound: 6	Cytotoxicity against human MIAPaCa2 cells assessed as decrease in cell growth measured after 72 hrs by MTT assay Cytotoxicity against human MIAPaCa2 cells assessed as decrease in cell growth measured after 72 hrs by MTT assay	[PMID: 31725297]
NCI-H460	IC₅₀	11.7 μM Compound: 2	Antiproliferative activity against human NCI-H460 cell line by MTT assay Antiproliferative activity against human NCI-H460 cell line by MTT assay	[PMID: 16970405]
PANC-1	IC₅₀	10 μM Compound: Zoledronate	Cytotoxicity against human PANC-1 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay Cytotoxicity against human PANC-1 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 33132173]
PANC-1	EC₅₀	16.1 μM Compound: 6	Cytotoxicity against human PANC1 cells assessed as decrease in cell growth measured after 72 hrs by MTT assay Cytotoxicity against human PANC1 cells assessed as decrease in cell growth measured after 72 hrs by MTT assay	[PMID: 31725297]
RPMI-8226	EC₅₀	11 μM Compound: 1; ZOL	Antiproliferative activity against human RPMI8226 cells after 72 hrs by MTT assay Antiproliferative activity against human RPMI8226 cells after 72 hrs by MTT assay	[PMID: 30016091]
RPMI-8226	EC₅₀	11 μM Compound: 1	Cytotoxicity against human RPMI8226 cells after 72 hrs by MTT assay Cytotoxicity against human RPMI8226 cells after 72 hrs by MTT assay	[PMID: 23998921]
SF-268	IC₅₀	14.3 μM Compound: 2	Antiproliferative activity against human SF-268 cell line by MTT assay Antiproliferative activity against human SF-268 cell line by MTT assay	[PMID: 16970405]
T-cell	IC₅₀	170 μM Compound: 1	Activation of human CD4+ Vgamma2/Vdelta2 T cell clone JN.23 assessed as TNF-alpha release after 16 hrs by sandwich ELISA in presence of antigen presenting cell line, CP.EBV Activation of human CD4+ Vgamma2/Vdelta2 T cell clone JN.23 assessed as TNF-alpha release after 16 hrs by sandwich ELISA in presence of antigen presenting cell line, CP.EBV	[PMID: 23610597]

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].

MCE 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].

MCE 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

性状

固体

颜色

White to off-white

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

细胞实验：

H₂O 中的溶解度 : 14.29 mg/mL (49.26 mM; ultrasonic and adjust pH to 8 with NaOH)

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

查看完整储备液配制表

* 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。

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。

方案一

请依序添加每种溶剂： PBS
Solubility: 3.33 mg/mL (11.48 mM); 澄清溶液; 超声助溶 (<60°C)

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

计算结果

工作液所需浓度 : mg/mL

您所需的储备液浓度超过该产品的实测溶解度，如有需要，请与 MCE 中国技术支持联系。

纯度 & 产品资料

纯度: 99.88%

选择批次：

Data Sheet (628 KB) SDS (393 KB)

COA (297 KB) RP-HPLC (258 KB)

产品使用指南 (1538 KB)

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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

[6]. Shea GKH, et al. Oral Zoledronic acid bisphosphonate for the treatment of chronic low back pain with associated Modic changes: A pilot randomized controlled trial. J Orthop Res. 2022 Feb 23. [Content Brief]

Zoledronic acid monohydrate 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

H₂O	1 mM	3.4471 mL	17.2354 mL	34.4709 mL	86.1772 mL
	5 mM	0.6894 mL	3.4471 mL	6.8942 mL	17.2354 mL
	10 mM	0.3447 mL	1.7235 mL	3.4471 mL	8.6177 mL
	15 mM	0.2298 mL	1.1490 mL	2.2981 mL	5.7451 mL
	20 mM	0.1724 mL	0.8618 mL	1.7235 mL	4.3089 mL
	25 mM	0.1379 mL	0.6894 mL	1.3788 mL	3.4471 mL
	30 mM	0.1149 mL	0.5745 mL	1.1490 mL	2.8726 mL
	40 mM	0.0862 mL	0.4309 mL	0.8618 mL	2.1544 mL

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

站点地图隐私声明

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上海工商

沪公网安备31011502019417

沪(浦)应急管危经许[2021]201709(QFYS)

营业执照（三证合一）

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

Customer Review

Other Forms of Zoledronic acid monohydrate:

MCE 顾客使用本产品发表的 12 篇科研文献