Zoledronic acid (Zoledronate)

別名: ZA, CGP-4244, GP42446A, ZOL 446 中文名稱：唑來膦酸

目錄號：S1314 Purity: 99.80%

Zoledronic acid (Zoledronate), 破骨細胞抑制劑，通過抑制甲羥戊酸途徑誘導破骨細胞凋亡，并防止小GTP結合蛋白，如Ras 和 Rho的異戊二烯化。Zoledronic acid (ZA) 還可誘導自噬。

Zoledronic acid (Zoledronate) Chemical Structure

CAS: 118072-93-8

規(guī)格	價格	庫存
25mg	564.29	現(xiàn)貨
100mg	1711.23	現(xiàn)貨
1g	5487.3	現(xiàn)貨
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產品質控

批次：純度： 99.80%

99.80

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細胞實驗數(shù)據示例

細胞系	實驗類型	給藥濃度	孵育時間	活性描述	文獻信息
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
點擊查看更多細胞系數(shù)據

生物活性

產品描述

靶點

Rho ^[1]
(Cell-free assay)

Ras ^[1]

體外研究(In Vitro)
體外研究活性	Zoledronic acid (10 µM和100 µM)引起MCF-7細胞按比例顯著減少(49.54% ，對照組23.55% ) (P < 0.05)。Zoledronic acid在0.1–10 µM濃度下對MDA-MB-231細胞影響很小，然而在100 µM濃度下會導致細胞數(shù)量顯著降低。Zoledronic acid (100 µM)在72小時時會引起MCF-7細胞數(shù)減少63.5%，在96小時時，會使其減少87.1%。Zoledronic acid (10 µM)會導致MCF-7細胞凋亡多于4倍的增加，而在100 µM濃度下，會使細胞凋亡的比例增加6倍。Zoledronic acid (10 µM) 和paclitaxel (2 µM)引起的細胞凋亡（對照組的774.8%）與單獨使用zoledronic acid（155.71%）相比增加了5倍，與單獨使用paclitaxel（189.68）相比，增加了4倍。Zoledronic acid誘導的MCF-7乳腺癌細胞凋亡會被甲羥戊酸途徑中間體的加入所抑制，這與在破骨細胞，巨噬細胞和骨髓瘤細胞中的情況相一致。^[1] Zoledronic acid劑量依賴性增強OPG基因的表達和人類成骨細胞（hOB）中蛋白質的分泌，在10 nM濃度下，72小時后有最大效果，這與Zoledronic acid更高的生物學效能相一致。Zoledronic acid阻止了人類成骨細胞中糖皮質激素dexamethasone對OPG mRNA和蛋白質合成的抑制作用。Zoledronic acid在人類成骨細胞中分別誘導2倍的I型膠原分泌和4倍的堿性磷酸酶活性。^[2]
實驗圖片	檢測方法	檢測指標	實驗圖片	PMID
	Western blot	ALDH1 / Oct4 / Nanog / Sox2 / CD49f N-cadherin / E-cadherin / Vimentin		30791957
	Growth inhibition assay	Cell viability		30791957

體內研究(In Vivo)
體內研究活性	在5T2MM小鼠體內，Zoledronic acid（120微克/千克，皮下注射）防止損傷的形成，防止松質骨和骨密度損失，并且減少破骨細胞的范圍。在5T2MM小鼠體內，Zoledronic acid（120毫克/千克，皮下注射）也減少了病變蛋白濃度和腫瘤負擔以及血管新生。^[3]

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試驗信息 (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

參考文獻
[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.

參考文獻

[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.

化學信息&溶解度

分子量	272.09	分子式	C₅H₁₀N₂O₇P₂
CAS號	118072-93-8	SDF	Download Zoledronic acid (Zoledronate) SDF
Smiles	C1=CN(C=N1)CC(O)(P(=O)(O)O)P(=O)(O)O
儲存條件(自收到貨起)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復凍融！	1年-80°C溶于溶劑
儲存條件(自收到貨起)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復凍融！	1個月-20°C溶于溶劑

體外溶解度
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吸濕會降低化合物溶解度，請使用新開封DMSO)

0.5MNAOH : 5.07 mg/mL (18.63 mM)

DMSO : Insoluble ( ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

摩爾濃度計算器

體內溶解度
批次：

現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑

動物體內配方計算器

實驗計算

摩爾濃度計算器

質量	濃度	體積	分子量
=	×	×

稀釋計算器分子量計算器

動物體內配方計算器（澄清溶液）

第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）

給藥劑量 mg/kg 動物平均體重 g 每只動物給藥體積 μL 動物數(shù)量只

第二步：請輸入動物體內配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

計算結果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；

體內配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH₂O，混勻澄清。

體內配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

技術支持

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操作手冊

如果有其他問題，請給我們留言。

* 必填項

常見問題及建議解決方法

問題 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):

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