BzATP triethylammonium salt
(Synonyms: 2-3-(4-苯甲酰苯甲酰)腺苷5-三磷酸三乙铵盐) 目录号 : GC15898
BzATP triethylammonium salt是一种强效的三磷酸腺苷（ATP）类似物，主要作为嘌呤能P2X受体发挥作用（EC50：大鼠P2X7 = 3.6μM；小鼠P2X7 = 285μM)。
Cas No.:112898-15-4
Sample solution is provided at 25 µL, 10mM.
BzATP triethylammonium salt is a potent adenosine triphosphate (ATP) analog that primarily acts as a purinergic P2X receptor (EC50：rat P2X7 = 3.6μM；mouse P2X7 = 285μM) [1]. BzATP triethylammonium salt activates the P2X7 receptor, opening nonselective cation channels on the cell membrane [2]. BzATP triethylammonium salt promotes Ca2⁺ and Na⁺ influx and K⁺ efflux, thereby inducing a cellular inflammatory signaling cascade, including NLRP3 inflammasome activation and the release of inflammatory cytokines such as IL-1β and IL-18 [3]. BzATP triethylammonium salt is commonly used to study physiological and pathological processes such as neuroinflammation, immunoregulation, and apoptosis [4].
In U87 glioma cells, BzATP triethylammonium salt (5-1000μM; 72h) promotes glioma cell proliferation by activating P2X7 receptors, leading to significantly enhanced cell activity and proliferation [5]. In A549 cells, BzATP triethylammonium salt (150-600μM; 72h) can inhibit cell proliferation and induce apoptosis, and its mechanism of action may be associated with promoting the release of TNF-α and inhibiting the NF-κB signaling pathway [6].
In 4T1 cells breast cancer-bearing mice model, BzATP triethylammonium salt (50μg/kg; ip; 7d) treatment significantly increased tumor weight, myeloid lymphocyte infiltration, and P2X7 expression at the protein and cellular levels [7]. In collagen-induced arthritis (CIA) mice model, BzATP triethylammonium salt (1mg/kg; ip; 20d) treatment restored the damaging effects of erastin and alleviated metabolic abnormalities [8].
References:
[1]. Bianchi B R, Lynch K J, Touma E, et al. Pharmacological characterization of recombinant human and rat P2X receptor subtypes[J]. European journal of pharmacology, 1999, 376(1-2): 127-138.
[2]. Young M T, Pelegrin P, Surprenant A. Amino acid residues in the P2X7 receptor that mediate differential sensitivity to ATP and BzATP[J]. Molecular pharmacology, 2007, 71(1): 92-100.
[3]. Anderson A, Waithe O Y, Seplovich G, et al. Regulation of BzATP‐Induced Blood–Brain Barrier Endothelial Cell Hyperpermeability by NLRP3 Inflammasome Inhibition[J]. Microcirculation, 2025, 32(3): e70006.
[4]. Shieh C H. The role of purinergic receptors in the regulation of mRNA expression and release of inflammatory cytokines in cultured primary mouse glia[D]. Dissertation, Universität Freiburg, 2014, 2014.
[5]. Ji Z, Xie Y, Guan Y, et al. Involvement of P2X7 receptor in proliferation and migration of human glioma cells[J]. BioMed research international, 2018, 2018(1): 8591397.
[6]. ZENG K, RU Q, XIONG Q, et al. Effect of P2X7R agonist BzATP on cell growth and apoptosis in non-small cell lung cancer A549 cells[J]. Journal of International Oncology, 2016: 321-325.
[7]. Yu X, Chen X, Tang X, et al. P2X7 blockade inhibits the growth of breast cancer in 4T1 breast cancer-bearing mice by NLRP3/caspase 1 pathway[J]. Archives of Medical Science, 2020, 16(1).
[8]. Ma Y, Li W, Niu S, et al. BzATP reverses ferroptosis-induced gut microbiota disorders in collagen-induced arthritis mice[J]. International Immunopharmacology, 2023, 124: 110885.
BzATP triethylammonium salt是一种强效的三磷酸腺苷（ATP）类似物，主要作为嘌呤能P2X受体发挥作用（EC50：大鼠P2X7 = 3.6μM；小鼠P2X7 = 285μM) [1]。BzATP triethylammonium salt可激活P2X7受体，打开细胞膜上的非选择性阳离子通道 [2]。BzATP triethylammonium salt促进Ca2⁺和Na⁺内流以及K⁺外流，从而诱导细胞炎症信号级联，包括NLRP3炎症小体激活和炎症细胞因子（如IL-1β和IL-18）的释放 [3]。BzATP triethylammonium salt常用于研究神经炎症、免疫调节和细胞凋亡等生理和病理过程 [4]。
在U87胶质瘤细胞中，BzATP triethylammonium salt（5-1000μM；72h）通过激活P2X7受体促进胶质瘤细胞增殖，导致细胞活性和增殖能力显著增强 [5]。在A549细胞中，BzATP triethylammonium salt（150-600μM；72h）能抑制细胞增殖、诱导细胞凋亡，其作用机制可能与促进TNF-α的释放、抑制NF-κB信号通路有关 [6]。
在4T1细胞乳腺癌荷瘤小鼠模型中，BzATP triethylammonium salt（50μg/kg；ip；7d）治疗在蛋白和细胞水平上显著增加肿瘤重量、髓系淋巴细胞浸润以及P2X7的表达 [7]。在胶原导性关节炎（CIA）小鼠模型中，BzATP triethylammonium salt（1mg/kg；ip；20d）治疗可恢复erastin的破坏作用并减轻代谢异常 [8]。
| Cell experiment [1]: | |
Cell lines | U87 glioma cells |
Preparation Method | U87 glioma cells were seeded at a density of 1 × 105/well in 24-well plates and cultured overnight. The culture medium was replaced with fresh medium supplemented with different concentrations of BzATP triethylammonium salt (5, 10, 50, 100, 500, and 1000μM). At the end of the treatment, 25μL of MTT solution (5mg/mL) was added to the cell culture and incubated at 37℃ for 3 hours. |
Reaction Conditions | 5-1000μM; 72h |
Applications | BzATP triethylammonium salt promotes glioma cell proliferation by activating P2X7 receptors, leading to significantly enhanced cell activity and proliferation. |
| Animal experiment [2]: | |
Animal models | 4T1 cells breast cancer-bearing mice model |
Preparation Method | In this study, 50 mice were randomly divided into a normal group, a sham-operated group, a control group, a BzATP triethylammonium salt group, and a BBG group, with 10 mice in each group. The sham-operated, control, BzATP triethylammonium salt, and BBG groups were all 4T1 breast cancer-bearing mice. The sham-operated group received no intervention, while the control group received an intraperitoneal injection of deionized water. The BzATP triethylammonium salt and BBG groups received interventions with BzATP triethylammonium salt and BBG, respectively. BzATP triethylammonium salt was dissolved in deionized water and injected intraperitoneally at a dose of 50μg/kg, 1 hour after inoculation of 4T1 breast cancer cells; BBG was injected intraperitoneally at a dose of 30mg/kg. All drugs were administered as a single dose, and the animals were sacrificed 7 days after administration for analysis. |
Dosage form | 50μg/kg; ip; 7d |
Applications | BzATP triethylammonium salt treatment significantly increased tumor weight, myeloid lymphocyte infiltration, and P2X7 expression at the protein and cellular levels. |
References: | |
| Cas No. | 112898-15-4 | SDF | |
| 别名 | 2-3-(4-苯甲酰苯甲酰)腺苷5-三磷酸三乙铵盐 | ||
| 化学名 | triethylamine ((2R,3S,4R,5R)-5-(6-amino-9H-purin-9-yl)-3-((4-benzoylbenzoyl)oxy)-4-hydroxytetrahydrofuran-2-yl)methyl triphosphate | ||
| Canonical SMILES | NC1=C(N=CN2[C@@]3([H])[C@@](O)([H])[C@@](OC(C4=CC=C(C(C5=CC=CC=C5)=O)C=C4)=O)([H])[C@@](O3)([H])COP(O)(OP(O)(OP(O)(O)=O)=O)=O)C2=NC=N1.CCN(CC)CC | ||
| 分子式 | C24 H24 N5 O15 P3 . C6 H15 N | 分子量 | 816.58 |
| 溶解度 | <5mM in Water | 储存条件 | Store at -20°C |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.2246 mL | 6.1231 mL | 12.2462 mL |
| 5 mM | 244.9 μL | 1.2246 mL | 2.4492 mL |
| 10 mM | 122.5 μL | 612.3 μL | 1.2246 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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