IF 11
PMID: 37215981 ↗2-APB
Catalog No.: GC17562Purity:>98.00%Synonyms: 2-Aminoethoxydiphenyl borate, 2-APB, NSC 17107
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.
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Cas No.: 524-95-8
10mM (in 1mL DMSO)In Stock
$24.00
1
5mgIn Stock
$21.00
1
10mgIn Stock
$28.00
1
25mgIn Stock
$42.00
1
50mgIn Stock
$54.00
1
100mgIn Stock
$70.00
1
| Pack Size | Price | Availability | Quantity | Action |
|---|---|---|---|---|
| 10mM (in 1mL DMSO) | $24.00 | In Stock | 1 | |
| 5mg | $21.00 | In Stock | 1 | |
| 10mg | $28.00 | In Stock | 1 | |
| 25mg | $42.00 | In Stock | 1 | |
| 50mg | $54.00 | In Stock | 1 | |
| 100mg | $70.00 | In Stock | 1 |
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Citations
4 publicationsPublications from researchers using this productDescription
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.
Protocol
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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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Product Documents
Purity:>98.00%Appearance:A solid
Biological Data
1 / 4
Chemical Properties
CAS No.
524-95-8
Synonyms
2-Aminoethoxydiphenyl borate, 2-APB, NSC 17107
Chemical Name
2-((diphenylboryl)oxy)ethanamine
SMILES
NCCOB(C1=CC=CC=C1)C2=CC=CC=C2
Molecular Formula
C14H16BNO
Molecular Weight
225.1
Solubility
≥ 9.4mg/mL in DMSO
Storage
Store at -20°C, protect from light
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.
CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility
g/mol
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