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(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。

BAPTA-AM Chemical Structure

Cas No.:126150-97-8

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥557.00
现货
10mg
¥515.00
现货
50mg
¥1,649.00
现货

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Description

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] 

实验参考方法

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.

化学性质

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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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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