2-APB
(Synonyms: 二苯基硼酸-2-氨基乙酯,2-APB) 目录号 : GC17562
2-APB是一种钙离子通道的非特异性拮抗剂，通常被用于研究钙信号传导，如细胞凋亡、肌肉收缩和神经传导等方面。
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.
2-APB是一种钙离子通道的非特异性拮抗剂，通常被用于研究钙信号传导，如细胞凋亡、肌肉收缩和神经传导等方面。2-APB是肌醇-1，4，5-三磷酸（InsP3）敏感性Ca2+通道的膜渗透性抑制剂，InsP3浓度为100 nm时，其IC50值为42μM[1]。此外，2-APB还被发现在一定浓度下能够影响TRP通道的活性[2]。
在体外，2-APB可以抑制凝血酶诱导的人类血小板和中性粒细胞胞内Ca2+增加，血管紧张素Ⅱ（AⅡ）诱导的胸主动脉收缩[1]。在HEK-293细胞中，2-APB阻断TRPC5通道，其IC50值为20 μM [3]。在小鼠胰腺腺泡细胞中，低浓度的2-APB可以显著抑制钙库调控的钙内流，高浓度的2-APB抑制直接刺激的Ca2+释放和InsP3诱导的Ca2+释放[4]。
在体内，2-APB以10 mg/kg静脉注射给予I/R模型小鼠时，2-APB能够显著减小梗塞面积，同时伴随着 ROS 水平和中性粒细胞浸润的减少，展现出潜在的心脏保护作用[5]。另外，在I/R大鼠中，2-APB显著增加超氧化物歧化酶（SOD）、总抗氧化能力（TAC）和谷胱甘肽（GSH），同时减少丙二醛（MDA）和DNA片段，2-APB具有抗凋亡和抗氧化作用[6]。
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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 | |
| 别名 | 二苯基硼酸-2-氨基乙酯,2-APB | ||
| 化学名 | 2-((diphenylboryl)oxy)ethanamine | ||
| Canonical SMILES | NCCOB(C1=CC=CC=C1)C2=CC=CC=C2 | ||
| 分子式 | C14H16BNO | 分子量 | 225.1 |
| 溶解度 | ≥ 9.4mg/mL in DMSO | 储存条件 | Store at -20°C, protect from light |
| 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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| 制备储备液 | |||
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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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动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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2.
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