BAPTA-AM (Synonyms: BAPTA Acetoxymethyl ester) |
| カタログ番号GC13517 |
BAPTA-AMは、広く知られた膜透過性のCa2+キレーターであり、細胞内のカルシウム過剰を緩和して細胞損傷を防ぐために使用される。
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Cas No.: 126150-97-8
Sample solution is provided at 25 µL, 10mM.
BAPTA-AMは、広く知られた膜透過性のCa2+キレーターであり、細胞内のカルシウム過剰を緩和して細胞損傷を防ぐために使用される。
BAPTA-AMのIC50値はMTTアッセイを用いて調査された。BAPTA-AMのIC50値は、乳がん細胞株4T1において13.6 µMと決定された。BortezomibとBAPTA-AMの併用効果を決定するために、細胞に対してさまざまな濃度のbortezomib（1 nMおよび10 nM）とBAPTA-AM（0.5および5 µM）を投与した。10 nMのbortezomib + 5 µMのBAPTA-AMの併用は、単剤療法（10 nMのbortezomibまたは5 µMのBAPTA-AM単独）よりも効果的であった。
カルシウムキレーターであるBAPTA-AMは、鉄過剰による軟骨細胞の損傷に対する治療効果を評価するために使用される。BAPTA-AMは、軟骨細胞中の鉄レベルを有意に低下させ、鉄過剰による細胞アポトーシスやMMPの発現を抑制した。これにより、鉄過剰関連疾患の治療に新たな知見が得られた。
BAPTA-AMによるIP3RとCa2+ホメオスタシスの回復は、高揚容量換気（HTV）による肺損傷と炎症を緩和することができる。BAPTA-AMの用量依存効果の評価では、2.5mg/kgがHTVによって誘発される過剰なER Ca2+放出を防ぐのに十分であることが示された。結果は組織病理学、W/D比、BALF蛋白レベル、浸潤細胞数、炎症性サイトカインIL-1β、IL-6、TNF-αレベルによって評価された。
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, Erdoğan 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.
| 細胞実験[1]: | |
細胞株 | 軟骨細胞 |
準備方法 | 軟骨細胞は100 µmのFACで処理され、BAPTA-AMを添加した場合もある。細胞内の鉄は0.5 mmのカルセイン-AMで染色され、共焦点顕微鏡で15分観察され、軟骨細胞内の二価鉄の取り込みと流出を評価した。 |
反応条件 | 10 µM BAPTA-AM; 3日間 |
アプリケーション | 鉄キレーターのBAPTA-AMは、軟骨細胞内での鉄の取り込みを抑制する。FAC処理群では蛍光強度が有意に低下し、軟骨細胞内の鉄含量が増加していることを示している。一方、BAPTA-AM共同処理群では蛍光強度が有意に増加し、軟骨細胞内の鉄濃度が低下していることを示している。 |
| 動物実験 [2]: | |
動物モデル | C57BL/6マウス |
準備方法 | マウスをCa2+キレーターであるBAPTA-AMで予処理した。肺組織と気管支肺洗浄液（BALF）が収集され、HTVに関連する過剰なER Ca2+の放出、炎症反応、およびERストレス、NLRP3インフラマソーム活性化、炎症に関連するmRNA /タンパク質発現が測定された。 |
投与形態 | 1.25、2.5、5mg/kg BAPTA-AM、腹腔内（i.p.）注射 |
アプリケーション | BAPTA-AMの投与による投与量依存的な効果の評価では、2.5mg/kgがHTVによって誘発される過剰なER Ca2+放出を防ぐのに十分であることが示された。BAPTA-AMによってHTVによる肺水腫と損傷が改善された。さらに、BALF中のIL-1β、IL-6、TNF-αの濃度はカルバコール存在下で有意に増加したが、BAPTA-AMはBALFのサイトカインレベルの増加を阻害した。 |
参考文献: [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 | |
| 同義語 | 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 | ||
| Formula | C34H40N2O18 | M.Wt | 764.68 |
| 溶解度 | ≥ 16.3mg/mL in DMSO with gentle warming | Storage | Desiccate at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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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- Purity: >99.00%
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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
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