BAPTA-AM
(Synonyms: BAPTA Acetoxymethyl ester) 目录号 : GC13517BAPTA-AM 是一种众所周知的可透过膜的 Ca2+ 螯合剂,可通过减轻细胞内钙过载来防止细胞损伤。
Cas No.:126150-97-8
Sample solution is provided at 25 µL, 10mM.
BAPTA-AM is a well-known membrane-permeable Ca2+ chelator, to prevent cell injury by allaying the intracellular calcium overload[1].
The IC50 value of BAPTA-AM was investigated using a MTT assay. The IC50 value of BAPTA-AM was determined as 13.6 μM in the breast cancer 4T1 cell line.In order to determine the combined effects of bortezomib and BAPTA-AM,The cells were treated with various doses of bortezomib (1 nM and 10 nM) and BAPTA-AM (0.5 and 5 μM). The combination of 10 nM bortezomib + 5 μM BAPTA-AM was more effective compared with monotherapies (10 nM bortezomib or 5 μM BAPTA-AM alone)[2]
The calcium chelator BAPTA-AM was used to test the efficacy of calcium chelator treatment in iron overload-induced chondrocyte damage. BAPTA-AM significantly reduced iron levels in chondrocytes and inhibited iron overload-induced cell apoptosis and the expression of MMPs, thus providing new insights into the treatment of iron overload-induced diseases[3]
Restoring IP3R and Ca2+ homeostasis by pretreatment with BAPTA-AM could alleviate HTV-induced lung injury and inflammation. Assessment of the dose-dependent effects of BAPTA-AM revealed that 2.5mg/kg was sufficient to prevent the excessive ER Ca2+ release induced by HTV. The results were assessed by histopathology, W/D ratio, BALF protein levels, the number of infiltrating cells and the levels of the inflammatory cytokines IL-1β, IL-6 and TNF-α[4]
References:
[1]. Fu Z, Fan Q, et al. Elimination of Intracellular Calcium Overload by BAPTA-AM-Loaded Liposomes: A Promising Therapeutic Agent for Acute Liver Failure. ACS Appl Mater Interfaces. 2019 Oct 30;11(43):39574-39585.
[2]. Yerlikaya A, Erdo?an E, et al. A novel combination treatment for breast cancer cells involving BAPTA-AM and proteasome inhibitor bortezomib. Oncol Lett. 2016 Jul;12(1):323-330.
[3]. Jing X, Wang Q, et al. Calcium chelator BAPTA AM protects against iron overload induced chondrocyte mitochondrial dysfunction and cartilage degeneration. Int J Mol Med. 2021 Oct;48(4):196.
[4]. Ye L, Zeng Q, et al.Inhibition of IP3R/Ca2+ Dysregulation Protects Mice From Ventilator-Induced Lung Injury via Endoplasmic Reticulum and Mitochondrial Pathways. Front Immunol. 2021 Sep 15;12:729094.
BAPTA-AM 是一种众所周知的可透过膜的 Ca2+ 螯合剂,可通过减轻细胞内钙过载来防止细胞损伤[1]。
使用 MTT 测定法研究了 BAPTA-AM 的 IC50 值。 BAPTA-AM 在乳腺癌 4T1 细胞系中的 IC50 值为 13.6 μM。硼替佐米(1 nM 和 10 nM)和 BAPTA-AM(0.5 和 5 μM)。与单一疗法(单独使用 10 nM 硼替佐米或 5 μM BAPTA-AM)相比,10 nM 硼替佐米 + 5 μM BAPTA-AM 的组合更有效[2]
钙螯合剂 BAPTA-AM 用于测试钙螯合剂治疗铁过载诱导的软骨细胞损伤的疗效。 BAPTA-AM显着降低软骨细胞铁含量,抑制铁超载诱导的细胞凋亡和MMPs的表达,为铁超载相关疾病的治疗提供新思路[3]
通过 BAPTA-AM 预处理恢复 IP3R 和 Ca2+ 稳态可减轻 HTV 引起的肺损伤和炎症。评估 BAPTA-AM 的剂量依赖性效应表明,2.5mg/kg 足以防止 HTV 诱导的 ER Ca2+ 过度释放。通过组织病理学、W/D 比值、BALF 蛋白水平、浸润细胞数量和炎性细胞因子 IL-1β、IL-6 和 TNF-α 水平评估结果[4]
Cell experiment [1]: | |
Cell lines |
Chondrocyte |
Preparation Method |
Chondrocytes were treated with 100 µm FAC, with or without BAPTA-AM. Intracellular iron was stained with 0.5 mm calcein-AM for 15 min and then observed by confocal microscopy to assess the ferrous iron uptake and outflow in chondrocytes |
Reaction Conditions |
10 µM BAPTA-AM for 3 days. |
Applications |
Iron chelator BAPTA-AM inhibits iron influx in chondrocytes.The fluorescence intensity significantly decreased in the FAC treatment group, indicating elevated iron content in chondrocytes. By contrast, the fluorescence intensity significantly increased in the BAPTA-AM co-treatment group, indicating that the BAPTA-AM co-treatment decreased iron concentration in chondrocytes. |
Animal experiment [2]: | |
Animal models |
C57BL/6 mice |
Preparation Method |
Mice were pretreated with the Ca2+ chelator BAPTA-AM. Lung tissues and bronchoalveolar lavage fluid (BALF) were collected to measure Ca2+ concentrations, inflammatory responses and mRNA/protein expression associated with ER stress, NLRP3 inflammasome activation and inflammation. |
Dosage form |
1.25, 2.5, 5mg/kg BAPTA-AM, intraperitoneal (i.p.) injection |
Applications |
Assessment of the dose-dependent effects of BAPTA-AM revealed that 2.5mg/kg was sufficient to prevent the excessive ER Ca2+ release induced by HTV .HTV-induced lung edema and injury were improved by treatment with BAPTA-AM. Consistently, the concentrations of IL-1β, IL-6 and TNF-α in BALF were significantly increased in the presence of carbachol, whereas BAPTA-AM blocked the increase in BALF cytokine levels. |
References: [1]. Jing X, Wang Q, et al.Calcium chelator BAPTA AM protects against iron overload induced chondrocyte mitochondrial dysfunction and cartilage degeneration. Int J Mol Med. 2021 Oct;48(4):196. [2]. Ye L, Zeng Q, et al.Inhibition of IP3R/Ca2+ Dysregulation Protects Mice From Ventilator-Induced Lung Injury via Endoplasmic Reticulum and Mitochondrial Pathways. Front Immunol. 2021 Sep 15;12:729094. |
Cas No. | 126150-97-8 | SDF | |
别名 | BAPTA Acetoxymethyl ester | ||
Canonical SMILES | O=C(CN(CC(OCOC(C)=O)=O)C1=CC=CC=C1OCCOC2=CC=CC=C2N(CC(OCOC(C)=O)=O)CC(OCOC(C)=O)=O)OCOC(C)=O | ||
分子式 | C34H40N2O18 | 分子量 | 764.68 |
溶解度 | ≥ 16.3mg/mL in DMSO with gentle warming | 储存条件 | Desiccate at -20°C |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 1.3077 mL | 6.5387 mL | 13.0774 mL |
5 mM | 0.2615 mL | 1.3077 mL | 2.6155 mL |
10 mM | 0.1308 mL | 0.6539 mL | 1.3077 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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2.
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Related Biological Data
Excessive intracellular Ca2+ concentration activates calpain to degrade the microtubule of N2a cells.(D) SK-N-SH cells were transfected with Vector or CVS-M-FLAG for 36 h or transfected with CVS-M-FLAG for 12 h and treated with BAPTA-AM (25 µM) for 24 h; lysates were analyzed by WB.
N2a cells were transfected with Vector or CVS-M-FLAG for 12 h; then, cells were treated with DMSO, EGTA-AM, BAPTA-AM (Glpbio) (25 µM), Calpain inhibitor III, or Z-VAD-FMK for 24 h; lysates were analyzed by WB.
Mbio (2024). PMID: 38349129 IF: 6.3996 -
Related Biological Data
Different dihydropyridine-derived calcium channel blockers inhibit HTNV infection. (C) Huh7 cells were infected with HTNV upon treatment with BAPTA-AM, 24 hpi.
The calcium chelator BAPTA-AM was purchased from GlpBio (Montclair, CA, United States).
Front Pharmacol 13 (2022): 940178. PMID: 36105208 IF: 5.6 -
Related Biological Data
The PLC/IP3R/STIM-dependent Ca2+ channel inhibitors attenuate histone-induced apoptosis and defective bacterial phagocytosis in macrophages. A–D The percentage of apoptotic cells was quantified by Annexin V-FITC/PI staining.
To explore the effect of BAPTA-AM on histone-induced macrophage damage in CLP mice, mice were pretreated intraperitoneally with BAPTA-AM (GlpBio) (7.5 mg/kg) for 30 min and then subjected to CLP, followed by intravenous injection of histones (20 mg/kg).
Int Immunopharmacol 132 (2024): 111870. PMID: 38547771 IF: 5.5999 -
Related Biological Data
Isoflurance preconditioning was involved in intracellular Ca2+ of liver macrophages. C. The activation of NF-KB in KCs was examined by laser scanning confocal microscope (600×).
BAPTA-AM (GLPBIO, USA), a selective calcium chelator, was used to inhibit intracellular Ca2+.
Int Immunopharmacol 99 (2021): 107977. PMID: 34332342 IF: 4.93 -
Related Biological Data
The effects of BAPTA-AM on the IP3R-MCU calcium regulation axis in GC-1 spg cells.GC-1 spg cells were pretreated with BAPTA-AM before CdCl2 exposure. The mRNA expression levels in GC-1 spg cells were detected by RT-PCR.
However, BAPTA-AM (GlpBio) (10μM or 15μM) significantly increased the viability of the GC-1spg cells inhibited by CdCl2.
Toxicology (2023): 153448. PMID: 36731763 IF: 4.571 -
Related Biological Data
Activation of Piezo1 promoted chondrocytes senescence through Ca2+ accumulation. A and B. Representative fluorescence imaging of intracellular Ca2+, ROS and mean fluorescence intensity of chondrocytes after Yoda1 or BAPTA-AM treatment.
When primary chondrocytes proliferated to 80% density, they were intervened with 5 mM Yoda1 with or without 10 mM BAPTA-AM (GLPBio, GC13517) for 24 h, as in the previous study.
Biochem Bioph Res Co (2022). PMID: 35367826 IF: 3.5753