Zoledronic acid (Zoledronate)

别名: ZA, CGP-4244, GP42446A, ZOL 446 中文名称：唑来膦酸

目录号：S1314 Purity: 99.80%

Zoledronic acid (Zoledronate), 破骨细胞抑制剂，通过抑制甲羟戊酸途径诱导破骨细胞凋亡，并防止小GTP结合蛋白，如Ras 和 Rho的异戊二烯化。Zoledronic acid (ZA) 还可诱导自噬。

Zoledronic acid (Zoledronate) Chemical Structure

CAS: 118072-93-8

规格	价格	库存
25mg	564.29	现货
100mg	1711.23	现货
1g	5487.3	现货
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产品质控

批次：纯度： 99.80%

99.80

Zoledronic acid (Zoledronate)相关产品

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细胞实验数据示例

细胞系	实验类型	给药浓度	孵育时间	活性描述	文献信息
J774A.1	Antiproliferative assay	100 uM	72 hrs	Antiproliferative activity against mouse J774A.1 cells assessed as reduction in cell viability at 100 uM after 72 hrs by WST8 assay	30216851
RAW264.7	Antiproliferative assay	100 uM	72 hrs	Antiproliferative activity against mouse RAW264.7 cells assessed as reduction in cell viability at 100 uM after 72 hrs by WST8 assay	30216851
MG63	Antiproliferative assay	100 uM	72 hrs	Antiproliferative activity against human MG63 cells assessed as reduction in cell viability at 100 uM after 72 hrs by WST8 assay	30216851
PC3	Antiproliferative assay	100 uM	72 hrs	Antiproliferative activity against human PC3 cells assessed as reduction in cell viability at 100 uM after 72 hrs by WST8 assay	30216851
RAW264.7	Antiproliferative assay	100 uM	72 hrs	Antiproliferative activity against RANKL-differentiated mouse RAW264.7 cells assessed as reduction in cell viability at 100 uM after 72 hrs by CCK8 assay	30216851
MC3T3-E1	Function assay	30 to 50 nM	10 to 15 days	Induction of mineralization in mouse MC3T3-E1 cells at 30 to 50 nM after 10 to 15 days by alizarin red dye based assay	30216851
C57BL mouse bone marrow cells	Function assay	50 nM	10 to 15 days	Induction of mineralization in C57BL mouse bone marrow cells at 50 nM supplemented with fresh medium containing compound every 3 days for 10 to 15 days by alizarin red dye based assay	30216851
C57BL mouse bone marrow cells/human PC3 cells	Function assay	50 to 100 nM	10 to 15 days	Induction of mineralization in C57BL mouse bone marrow cells co-cultured with human PC3 cells at 50 to 100 nM supplemented with fresh medium containing compound every 3 days for 10 to 15 days by alizarin red dye based assay	30216851
RPMI8226	Function assay	0.5 uM		Inhibition of GGPPS in human RPMI8226 cells assessed as reduction in Rap1A prenylation at 0.5 uM by Western blot analysis	30016091
BL21(DE3)	Function assay		30 mins	Inhibition of His6-tagged human truncated FPPS (6-353) expressed in Escherichia coli BL21(DE3) cells using geranyl diphosphate and isopentenyl diphosphate as substrate preincubated with enzyme for 30 mins by spectrophotometric analysis, IC50=0.1μM	23610597
BL2-codon plus (DE3) RIL	Function assay		30 mins	Inhibition of N-terminal His6-tagged Plasmodium vivax GGPPS expressed in Escherichia coli BL2-codon plus (DE3) RIL cells using geranyl diphosphate and isopentenyl diphosphate as substrate preincubated with enzyme for 30 mins by spectrophotometric analysis, IC50=0.13μM	23610597
RPMI8226	Cytotoxicity assay		72 hrs	Cytotoxicity against human RPMI8226 cells after 72 hrs by MTT assay, EC50=11μM	23998921
MCF7	Antiproliferative assay		72 hrs	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50=23μM	24928399
Vgamma9/Vdelta2 T-cells	Function assay		18 hrs	Binding affinity to butyrophilin 3A1 in human Vgamma9/Vdelta2 T-cells assessed as activation of Vgamma9/Vdelta2 T-cells by upregulation of CD69 and CD25 after 18 hrs, EC50=0.4866μM	29457898
RPMI8226	Antiproliferative assay		72 hrs	Antiproliferative activity against human RPMI8226 cells after 72 hrs by MTT assay, EC50=11μM	30016091
RAW264.7	Function assay		72 hrs	Inhibition of RANKL-induced osteoclastogenesis in mouse RAW264.7 cells after 72 hrs by TRAP staining based microscopic analysis	30216851
K562	Function assay		240 mins	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, EC50=23μM	31531198
MIAPaCa2	Cytotoxicity assay		72 hrs	Cytotoxicity against human MIAPaCa2 cells assessed as decrease in cell growth measured after 72 hrs by MTT assay, EC50=13.4μM	31725297
PANC1	Cytotoxicity assay		72 hrs	Cytotoxicity against human PANC1 cells assessed as decrease in cell growth measured after 72 hrs by MTT assay, EC50=16.1μM	31725297
HFF cells	Function assay			Inhibitory concentration against the growth of Toxoplasma gondii overexpressing FPPS enzyme in human foreskin fibroblast monolayer cells; (control = 0.60 uM, experiment 1), IC50=7.8μM	15857119
HFF cells	Function assay			In vitro inhibitory concentration against the growth of Toxoplasma gondii in human foreskin fibroblast monolayer cells (HFF cells), IC50=0.79μM	15857119
Gamma delta T cells	Function assay			Effective concentration against human Gamma delta T cells, EC50=5.4μM	15828834
human SF-268 cell	Proliferation assay			Antiproliferative activity against human SF-268 cell line by MTT assay, IC50=14.3 μM	16970405
human NCI-H460 cell	Proliferation assay			Antiproliferative activity against human NCI-H460 cell line by MTT assay, IC50=11.7 μM	16970405
HFF cells	Function assay			Inhibitory concentration against the growth of Toxoplasma gondii overexpressing FPPS enzyme in human foreskin fibroblast monolayer cells; (control = 0.79 uM, experiment 3), IC50=7.8μM	15857119
HFF cells	Function assay			Inhibitory concentration against the growth of Toxoplasma gondii overexpressing FPPS enzyme in human foreskin fibroblast monolayer cells; (control = 1.1 uM, experiment 2), IC50=8.3μM	15857119
BT-549	Antitumor assay			Antitumor activity against human BT-549 cells xenografted SCID mouse co-transfected with human gamma delta T lymphocytes assessed as survival time prolongation at 2 ug, ip coadministered with human recombinant IL2	18937434
BT-549	Antitumor assay			Antitumor activity against human BT-549 cells xenografted SCID mouse co-transfected with human gamma delta T lymphocytes assessed as survival time prolongation at 5 ug, ip coadministered with human recombinant IL2	18937434
J774	Cytotoxicity assay			Cytotoxicity against mouse J774 cells assessed as reduction in cell viability, IC50=7.8μM	24813742
点击查看更多细胞系数据

生物活性

产品描述

靶点

Rho ^[1]
(Cell-free assay)

Ras ^[1]

体外研究(In Vitro)
体外研究活性	Zoledronic acid (10 µM和100 µM)引起MCF-7细胞按比例显著减少(49.54% ，对照组23.55% ) (P < 0.05)。Zoledronic acid在0.1–10 µM浓度下对MDA-MB-231细胞影响很小，然而在100 µM浓度下会导致细胞数量显著降低。Zoledronic acid (100 µM)在72小时时会引起MCF-7细胞数减少63.5%，在96小时时，会使其减少87.1%。Zoledronic acid (10 µM)会导致MCF-7细胞凋亡多于4倍的增加，而在100 µM浓度下，会使细胞凋亡的比例增加6倍。Zoledronic acid (10 µM) 和paclitaxel (2 µM)引起的细胞凋亡（对照组的774.8%）与单独使用zoledronic acid（155.71%）相比增加了5倍，与单独使用paclitaxel（189.68）相比，增加了4倍。Zoledronic acid诱导的MCF-7乳腺癌细胞凋亡会被甲羟戊酸途径中间体的加入所抑制，这与在破骨细胞，巨噬细胞和骨髓瘤细胞中的情况相一致。^[1] Zoledronic acid剂量依赖性增强OPG基因的表达和人类成骨细胞（hOB）中蛋白质的分泌，在10 nM浓度下，72小时后有最大效果，这与Zoledronic acid更高的生物学效能相一致。Zoledronic acid阻止了人类成骨细胞中糖皮质激素dexamethasone对OPG mRNA和蛋白质合成的抑制作用。Zoledronic acid在人类成骨细胞中分别诱导2倍的I型胶原分泌和4倍的碱性磷酸酶活性。^[2]
实验图片	检测方法	检测指标	实验图片	PMID
	Western blot	ALDH1 / Oct4 / Nanog / Sox2 / CD49f N-cadherin / E-cadherin / Vimentin		30791957
	Growth inhibition assay	Cell viability		30791957

体内研究(In Vivo)
体内研究活性	在5T2MM小鼠体内，Zoledronic acid（120微克/千克，皮下注射）防止损伤的形成，防止松质骨和骨密度损失，并且减少破骨细胞的范围。在5T2MM小鼠体内，Zoledronic acid（120毫克/千克，皮下注射）也减少了病变蛋白浓度和肿瘤负担以及血管新生。^[3]

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
临床试验信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT06217718	Not yet recruiting	Copd\|Empowerment\|Empowerment Patient\|Self Efficacy	Zahide Aksoy\|The Scientific and Technological Research Council of Turkey\|Marmara University	February 15 2024	Not Applicable
NCT05743179	Recruiting	Hip Fractures\|Pneumonia	The University of Hong Kong\|Queen Mary Hospital Hong Kong\|Caritas Medical Centre Hong Kong\|Prince of Wales Hospital Shatin Hong Kong\|United Christian Hospital	December 5 2022	Phase 4
NCT02864784	Withdrawn	Castrate Resistant Prostate Cancer With Bone Metastasis	Amorphical Ltd.	June 2022	Phase 1
NCT04957641	Completed	Hereditary Angioedema	Takeda	April 21 2022	--
NCT05213286	Unknown status	Autism Spectrum Disorder\|Schizotypal Disorder	Glostrup University Hospital Copenhagen	February 1 2022	Not Applicable

参考文献
[1] Jagdev SP, et al. Br J Cancer, 2001, 84(8), 1126-1134. [2] Viereck V, et al. Biochem Biophys Res Commun, 2002, 291(3), 680-686. [3] Croucher PI, et al. J Bone Miner Res, 2003, 18(3), 482-492.

参考文献

化学信息&溶解度

分子量	272.09	分子式	C₅H₁₀N₂O₇P₂
CAS号	118072-93-8	SDF	Download Zoledronic acid (Zoledronate) SDF
Smiles	C1=CN(C=N1)CC(O)(P(=O)(O)O)P(=O)(O)O
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1年-80°C溶于溶剂
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1个月-20°C溶于溶剂

体外溶解度
批次：

0.1M NAOH : 25 mg/mL (91.88 mM)

Water : 0.5 mg/mL (1.83 mM) Warmed with 50°C water bath; Ultrasonicated;

DMSO : Insoluble ( ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

0.5MNAOH : 5.07 mg/mL (18.63 mM)

DMSO : Insoluble ( ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : Insoluble

摩尔浓度计算器

体内溶解度
批次：

现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×

稀释计算器分子量计算器

动物体内配方计算器（澄清溶液）

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 μL 动物数量只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

计算结果：

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH₂O，混匀澄清。

体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。

注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

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操作手册

如果有其他问题，请给我们留言。

* 必填项

常见问题及建议解决方法

问题 1:
How can I reconstitute the compound for in vivo studies?

回答：
Please dissolve this compound directly to 30% PEG400+0.5% Tween80+5% Propylene glycol.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):