2-APB (Synonyms: 2-Aminoethoxydiphenyl borate, 2-APB, NSC 17107) |
| Catalog No.GC17562 |
2-APB is a nonspecific antagonist of calcium channels, commonly used in studies of calcium signaling, such as in apoptosis, muscle contraction, and neural transmission.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 524-95-8
Sample solution is provided at 25 µL, 10mM.
2-APB is a nonspecific antagonist of calcium channels, commonly used in studies of calcium signaling, such as in apoptosis, muscle contraction, and neural transmission. It is a membrane-permeable inhibitor of the inositol-1,4,5-trisphosphate (InsP3) sensitive Ca2+ channels, with an IC50 value of 42μM when the concentration of InsP3 is 100nm[1]. Additionally, 2-APB has been found to affect the activity of TRP channels at certain concentrations [2].
In vitro, 2-APB can inhibit the increase in intracellular Ca2+ induced by thrombin in human platelets and neutrophils, as well as angiotensin II (AII)-induced contraction of the thoracic aorta [1]. In HEK-293 cells, 2-APB blocks the TRPC5 channel with an IC50 value of 20 μM [3]. In mouse pancreatic acinar cells, low concentrations of 2-APB significantly inhibit calcium store-operated calcium influx, while high concentrations inhibit direct stimulation-induced Ca2+ release and InsP3-induced Ca2+ release [4].
In vivo, when 2-APB is administered intravenously at 10 mg/kg to mice in an I/R model, it significantly reduces the infarct size, accompanied by a reduction in ROS levels and neutrophil infiltration, demonstrating potential cardioprotective effects [5]. Additionally, in I/R rats, 2-APB significantly increases superoxide dismutase (SOD), total antioxidant capacity (TAC), and glutathione (GSH), while reducing malondialdehyde (MDA) and DNA fragmentation, indicating that 2-APB has anti-apoptotic and antioxidative effects [6].
References:
[1]. Maruyama T, Kanaji T, Nakade S, et al. 2APB, 2-aminoethoxydiphenyl borate, a membrane-penetrable modulator of Ins(1,4,5)P3-induced Ca2+ release. J Biochem, 1997, 122(3): 498-505..
[2]. Togashi K , Inada H , Tominaga M .Inhibition of the transient receptor potential cation channel TRPM2 by 2-aminoethoxydiphenyl borate (2-APB)[J].British Journal of Pharmacology, 2008.
[3].Xu SZ, Zeng F, Boulay G, et al. Block of TRPC5 channels by 2-aminoethoxydiphenyl borate: a differential, extracellular and voltage-dependent effect. Br J Pharmacol, 2005, 145(4): 405-414.
[4]. Choi KJ, Kim KS, Kim SH, et al. Caffeine and 2-Aminoethoxydiphenyl Borate (2-APB) Have Different Ability to Inhibit Intracellular Calcium Mobilization in Pancreatic Acinar Cell. Korean J Physiol Pharmacol, 2010, 14(2): 105-111.
[5]. Hirofumi M , Masanori O , Shota T ,et al.2-aminoethoxydiphenyl borate provides an anti-oxidative effect and mediates cardioprotection during ischemia reperfusion in mice[J].Plos One, 2017, 12(12).
[6]. Sari E, Aksit H, Erken HA, et al. Protective effect of 2-APB on testicular ischemia-reperfusion injury in rats. J Urol, 2015, 193(3): 1036-1041.
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Cell experiment [1]: |
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Cell lines |
HEK293 cells |
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Preparation method |
HEK-293 cells were grown in DMEM-F12 medium containing 10% fetal calf serum, 100 U ml−1 penicillin, and 100 μg ml−1 streptomycin. The cells were first induced with 1 μg ml−1 tetracycline (Tet+) for 24-72 hours to express TRPC5 and TRPM2. Uninduced cells without addition of tetracycline (Tet−) were used as control. HEK-293 cells were incubated with 75 μ m 2-APB for 36–72 h. |
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Reaction Conditions |
75 μm; 36-72 h |
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Applications |
whole-cell current at −80 mV inhibited by 75 μm 2-APB in Tet+ (n=9) and Tet− (n=7) cells |
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Animal experiment [2]: |
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Animal models |
C57BL/6 male mice（I/R model） |
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Preparation method |
In the experiment conducted on C57BL/6 male mice (aged 7-9 weeks), isoflurane (1.5%) was used for anesthesia, and a myocardial ischemia-reperfusion (I/R) model was simulated through thoracotomy. The procedure included the temporary ligation of the left coronary artery to induce myocardial ischemia, followed by the release of the ligature for reperfusion. Prior to ischemia, mice in the 2-APB group received an intravenous injection of 10 mg/kg 2-APB (calculated as 125 μL saline/25 g body weight), while the control group received an equivalent volume of saline containing the vehicle. At the end of the experiment, myocardial infarct areas were assessed using Evans blue dye and 2% triphenyltetrazolium chloride staining, and analyzed using ImageJ software. |
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Dosage form |
10 mg/kg (indicated concentrations in 125 μL of saline / 25 g of body weight)；i.v. |
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Applications |
treatment with 2-APB led to a considerable reduction in the infarct size after I/R, which was accompanied by the reduction in ROS levels and neutrophil infiltration |
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References: [1]. Xu SZ, Zeng F, Boulay G, et al. Block of TRPC5 channels by 2-aminoethoxydiphenyl borate: a differential, extracellular and voltage-dependent effect. Br J Pharmacol, 2005, 145(4): 405-414. [2]. Hirofumi M , Masanori O , Shota T ,et al.2-aminoethoxydiphenyl borate provides an anti-oxidative effect and mediates cardioprotection during ischemia reperfusion in mice[J].Plos One, 2017, 12(12). |
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| Cas No. | 524-95-8 | SDF | |
| Synonyms | 2-Aminoethoxydiphenyl borate, 2-APB, NSC 17107 | ||
| Chemical Name | 2-((diphenylboryl)oxy)ethanamine | ||
| Canonical SMILES | NCCOB(C1=CC=CC=C1)C2=CC=CC=C2 | ||
| Formula | C14H16BNO | M.Wt | 225.1 |
| Solubility | ≥ 9.4mg/mL in DMSO | Storage | Store at -20°C, protect from light |
| 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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.4425 mL | 22.2124 mL | 44.4247 mL |
| 5 mM | 0.8885 mL | 4.4425 mL | 8.8849 mL |
| 10 mM | 0.4442 mL | 2.2212 mL | 4.4425 mL |
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- Purity: >98.00%
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Related Biological Data
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For T1D+SCI+2-APB group, 3 mg/kg of 2-APB (Glpbio) was intraperitioneally injected into rat daily from 1 day before SCI surgery to inhibit TRPM2 expression.
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ER-Mito calcium transport mediated mitochondrial fission and mitophagy.Western blot assays demonstrated that 2APB treatment resulted in notable decreases in the phosphorylation of Drp1 at Ser616 and increases in the expression of Mfn2 on soft substrates.
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Related Biological Data
Expression of CVS-M or infection with CVS leads to leakage of Ca2+ from intracellular Ca2+ pools and morphology change of the ER.We treated CVS-M-FLAG-expressing cells with 2-APB, an inhibitor of endoplasmic reticulum Ca2+ channels, and found that 2-APB treatment did not fully reverse the increase in Ca2+ concentration induced by CVS-M-FLAG expression.
N2a cells were cultured in Ca2+-free medium and transfected with Vector or CVS-M-FLAG and then were treated with DMSO or 2-APB(Glpbio) (50 µM) at 12 h post-transfection.
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Related Biological Data
IP3 receptor antagonists 2-APB mimicked the anti-inflammatory activity of PRE-084.2-APB reversed that elevated effect of LPS on calcineurin.
BV-2 microglia were pretreated with 2-APB(GlpBio) for 30 min, and then treated with LPS (200 ng/mL).
Neurochem Res 47.2 (2022): 264-278. PMID: 34468932 IF: 4.3997
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