BAPTA-AM
(Synonyms: BAPTA Acetoxymethyl ester) 目录号 : GC13517
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。
Cas No.:126150-97-8
Sample solution is provided at 25 µL, 10mM.
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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
Quality Control & SDS
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- Purity: >99.00%
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- Datasheet
| Cell experiment [1]: | |
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Cell lines |
Chondrocyte |
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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 |
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Reaction Conditions |
10 µM BAPTA-AM for 3 days. |
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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]: | |
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Animal models |
C57BL/6 mice |
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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. |
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Dosage form |
1.25, 2.5, 5mg/kg BAPTA-AM, intraperitoneal (i.p.) injection |
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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. |
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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. |
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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]
| 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 |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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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 | |||
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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 |
| 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 | ul | |
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GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
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，
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 saline，混匀澄清。
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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Calcium chelator BAPTA‑AM protects against iron overload‑induced chondrocyte mitochondrial dysfunction and cartilage degeneration
Int J Mol Med2021 Oct;48(4):196.PMID: 34468013DOI: 10.3892/ijmm.2021.5029
Osteoarthritis (OA) is a common joint disease that is characterized by cartilage degradation. Iron deposition in the joints is common during the pathogenic progression of OA and recent studies have indicated that iron overload is an important contributor to OA progression. Calcium chelators have been reported to inhibit iron influx via modulating transferrin receptor protein 1 internalization, and they have been identified as a potential approach to the treatment of iron overload‑induced diseases. The aim of the present study was to investigate the effect of calcium chelators on the progression of iron overload‑induced OA. Primary chondrocytes were treated with various concentrations of ferric ammonium citrate (FAC) to mimic iron overload in vitro, followed by co‑treatment with the calcium chelator BAPTA acetoxymethyl ester (BAPTA‑AM). Subsequently, intracellular iron levels, cell viability, reactive oxygen species (ROS) levels, mitochondrial function and morphological changes, as well as MMP levels, were detected using commercial kits. It was demonstrated that FAC treatment significantly promoted chondrocyte apoptosis and the expression of MMPs, and these effects were reversed by co‑treatment with BAPTA‑AM. Moreover, BAPTA‑AM suppressed iron influx into chondrocytes and inhibited iron overload‑induced ROS production and mitochondrial dysfunction. These results indicated that calcium chelators may be of value in the treatment of iron metabolism‑related diseases and iron overload‑induced OA progression.
BAPTA-AM dramatically improves maturation and development of bovine oocytes from grade-3 cumulus-oocyte complexes
Mol Reprod Dev2018 Jan;85(1):38-45.PMID: 29205619DOI: 10.1002/mrd.22936
Intracellular free calcium ([Ca2+ ]i ) is essential for oocyte maturation and early embryonic development. Here, we investigated the role of [Ca2+ ]i in oocytes from cumulus-oocyte complexes (COCs) with respect to maturation and early embryonic development, using the calcium-buffering agent BAPTA-AM (1,2-bis[2-aminophenoxy]ethane-N,N,N',N'-tetraacetic acid tetrakis [acetoxymethyl ester]). COCs were graded based on compactness of the cumulus mass and appearance of the cytoplasm, with Grade 1 indicating higher quality and developmental potential than Grade 3. Results showed that: (i) [Ca2+ ]i in metaphase-II (MII) oocytes from Grade-3 COCs was significantly higher than those from Grade-1 COCs, and was significantly reduced by BAPTA-AM; (ii) nuclear maturation of oocytes from Grade-3 COCs treated with BAPTA-AM was enhanced compared to untreated COCs; (iii) protein abundance of Cyclin B and oocyte-specific Histone 1 (H1FOO) was improved in MII oocytes from Grade-3 COCs treated with BAPTA-AM; (iv) Ca2+ transients were triggered in each group upon fertilization, and the amplitude of [Ca2+ ]i oscillations increased in the Grade-3 group upon treatment with BAPTA-AM, with the magnitude approaching that of the Grade-1 group; and (v) cleavage rates and blastocyst-formation rates were improved in the Grade-3 group treated with BAPTA-AM compared to untreated controls following in vitro fertilization and parthenogenetic activation. Therefore, BAPTA-AM dramatically improved oocyte maturation, oocyte quality, and embryonic development of oocytes from Grade-3 COCs.
Intracellular calcium chelating agent (BAPTA-AM) aids stallion semen cooling and freezing-thawing
Reprod Domest Anim2018 Oct;53(5):1235-1242.PMID: 29984866DOI: 10.1111/rda.13245
This study aimed to investigate the effects of different concentrations of 1,2-bis-(o-aminophenoxy)-ethane-N,N,N0 N0-tetraacetic acid, tetra-acetoxymethyl ester (BAPTA-AM), an intracellular calcium chelating agent, on stallion semen cooling and freezing-thawing. After collection, semen was extended (1:1 v/v) on a skim milk-based extender, centrifuged and resuspended at 400 million/ml into cooling or freezing extenders containing 0, 5, 25, 50, 100 and 200 μΜ BAPTA-AM. Motility parameters were assessed after cooling in Equitainer at 5°C for 12, 24, 48, 72 and 120 hr and after freezing-thawing. In addition, mitochondrial membrane potential, intracellular ATP, reactive oxygen species and malondialdehyde concentrations were measured in cryopreserved-thawed semen. Cooled stored (48 hr) semen containing 50 μΜ BAPTA-AM and control extender (0 μΜ BAPTA-AM) was used to assess fertility. Inclusion of 50 μΜ BAPTA-AM resulted in superior sperm motility parameters during cooled storage when compared to other groups (p < 0.05). Furthermore, semen cryopreserved in extender containing 50 μΜ BAPTA-AM showed increased intracellular ATP and mitochondrial membrane potential, whereas reactive oxygen species and malondialdehyde were increased after thawing for all groups (p < 0.05). Addition of 50 μΜ BAPTA-AM to cooling extender resulted in similar pregnancy rates to the control group (75% vs. 73.6%, respectively; p > 0.05). In conclusion, the addition of BAPTA-AM to semen extenders aided stallion semen cryopreservation in a dose-dependent manner. Furthermore, the cooling extender supplemented with 50 μΜ BAPTA-AM could be used to prolong the sperm motility during cooling without apparently compromising fertility. Field trials should be conducted to assess fertility of cryopreserved stallion semen with BAPTA-AM.
BAPTA-AM Nanoparticle for the Curing of Acute Kidney Injury Induced by Ischemia/Reperfusion
J Biomed Nanotechnol2018 May 1;14(5):868-883.PMID: 29883558DOI: 10.1166/jbn.2018.2532
Ischemia-reperfusion (I/R) is a major cause of acute kidney injury (AKI), which is associated with unacceptably high mortality rates in ICU. This research was designed to explore the therapeutic effect of BAPTA-AM (1,2-Bis(2-aminophenoxy) ethane-N,N,N,N-tetraacetic acid tetrakis(acetoxymethyl ester)) nanoparticle (BA-N) on AKI. BA-N was developed by liposome strategy and characterized by standard methods. The rat model was selected and the rats were randomly allocated into four groups: (1) Normal group; (2) Sham-operated group; (3) Model group (I/R + NS); (4) BA-N treatment group (I/R + BA-N). AKI model was established via clipping the bilateral renal artery with a microvascular clamp for 45 min. After reperfusion, serum cystatin C (Cys C), creatinine (Cr), blood urea nitrogen (BUN), lactate dehydrogenase (LDH) and caspase 3 levels were determined for the assessment of renal function. Kidney samples were then collected for the measurement of renal malondialdehyde (MDA) level and superoxide dismutase (SOD) activity. The assays of histological examination, ELISA, immunohistochemistry, western blot, TUNEL and RT-PCR were utilized for the detection of apoptosis. The results demonstrated that AKI model caused a significant decreasing in SOD activity, accompanied by a remarkable increase in Cys C, Cr, BUN, LDH, MDA, caspase 3 and cytochrome c (Cyt C) level, compared to the control group. BA-N (100 μg/kg i.v.) significantly improved renal function and histopathological appearance, restored MDA level and SOD activity, decreased Bax/Bcl-2 ratio, caspase 3 activity, Cyt C release and TUNEL positive apoptotic cells. Our studies indicated that BA-N plays a renal-protective role, probably through antiapoptotic and antioxidant mechanisms. BA-N may regulate mitochondria pathway via decreasing Bax/Bcl-2 ratio, inhibiting caspase 3 expression and Cyt C release. Overall, BA-N may have potentials as an anti-AKI drug.
Determination of BAPTA-AM, the acetoxymethyl tetraester of BAPTA, in rat plasma by liquid chromatography tandem mass spectrometry
J Mass Spectrom2006 Dec;41(12):1615-22.PMID: 17103492DOI: 10.1002/jms.1125
BAPTA-AM is the acetoxymethylester of the calcium chelator BAPTA and has demonstrated efficacy in several animal models of cerebral ischemia. This paper describes the development of a method for the determination of BAPTA-AM in rat plasma by liquid chromatography/tandem mass spectrometry. Owing to multiple ester groups in the structure of BAPTA-AM, [M + Na](+) was chosen as the analytical ion for quantification of BAPTA-AM. During the analytical method development, a high percentage of organic solvent and the addition of an amount of sodium acetate and formic acid in the mobile phase were found to favor the sensitivity and reproducibility of [M + Na](+). Poor fragmentation was usually observed in the MS/MS spectra of sodium adduct ions. However, abundant and reproducible fragment ions were observed for the BAPTA-AM sodium adduct ion, and therefore the traditional selective reaction-monitoring mode was used to further improve the sensitivity of MS detection. Because of the lability of the ester bond, a combination of fluoride and hydrochloric acid was applied to minimize the enzymatic hydrolysis, and acetonitrile was chosen to avoid the chemical hydrolysis or solvolysis during the sample collection and preparation procedure. On the basis of these studies, a rapid, sensitive and reproducible method for the determination of BAPTA-AM in rat plasma, using LC/ESI-MS/MS and a simple protein precipitation procedure, was developed and validated. Also, the present method was successfully applied to the determination of BAPTA-AM plasma concentrations for pharmacokinetic studies in rats.