2-APB
2-APB is an antagonist of Ins(1,4,5) P3-induced Ca2+ release with IC50 value of 42 μM [1].
Myo-Ins(1,4,5) P3 receptors (IP3R) mediates the mobilization of internal Ca2+. IP3R is involved in Ca2+ waves and Ca2+ oscillations.
2-APB is an antagonist of Ins(1,4,5) P3-induced Ca2+ release. 2APB inhibited Ins(1,4,5)-P3-induced Ca2+ release from rat cerebellar microsomal with IC50 value of 42 μM. Addition of 2APB to the extracellular inhibited the cytosolic Ca2+ rise in human platelets and neutrophils stimulated by thrombin. Also, 2APB inhibited the contraction of thoracic aorta induced by angiotensin II (AII) [1]. In HEK-293 cells, 2-APB in the extracellular blocked human TRPC5 channels with IC50 value of 20 μM. Also, 2-APB blocked TRPC6 and TRPM3. In cells overexpressing TRPC5, 2-APB inhibited cell proliferation [2]. In the mouse pancreatic acinar cell, 2-APB significantly inhibited store-operated Ca2+ (SOC)-mediated Ca2+ entry at low concentrations. In permeabilized acinar cell, 2-APB inhibited direct stimulation of Ca2+ release and InsP3-induced Ca2+ release at high concentrations [3].
In rats with I/R-induced testicular injury, 2-APB significantly increased superoxide dismutase (SOD), total antioxidant capacity (TAC) and glutathione (GSH) and reduced malondialdehyde (MDA) and DNA fragmentation, which suggested the antiapoptotic and antioxidative effects of 2-APB [4].
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]. 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.
[3]. 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.
[4]. 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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- 2. Hui Liu, Xuenan Li, et al. "Elaidic acid leads to mitochondrial dysfunction via mitochondria-associated membranes triggers disruption of mitochondrial calcium fluxes." Food Science and Human Wellness Volume 13 Issue 1, January 2024
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| Physical Appearance | A solid |
| Storage | Store at RT |
| M.Wt | 225.1 |
| Cas No. | 524-95-8 |
| Formula | C14H16BNO |
| Solubility | insoluble in H2O; ≥27.85 mg/mL in EtOH; ≥9.4 mg/mL in DMSO |
| Chemical Name | 2-((diphenylboryl)oxy)ethanamine |
| SDF | Download SDF |
| Canonical SMILES | NCCOB(C1=CC=CC=C1)C2=CC=CC=C2 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment:[1] | |
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Cell lines |
Mouse pancreatic acinar cells |
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Reaction Conditions |
10 ~ 100 μM 2-APB |
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Applications |
In mouse pancreatic acinar cells, 2-APB significantly inhibited store-operated Ca2+ (SOC) channel-mediated Ca2+ entry at low concentrations (~ 30 μM). At higher concentrations (~ 100 μM), 2-APB exerted multiple paradoxical effects including inhibition of InsP3-induced Ca2+ release and direct stimulation of Ca2+ release. |
| Animal experiment:[2] | |
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Animal models |
Adult male Sprague-Dawley rats, 250 ~ 300 g |
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Dosage form |
2 or 4 mg/kg Administered intraperitoneally |
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Applications |
In rats with ischemia-reperfusion (I/R) induced testicular injury, 2-APB significantly increased mean levels of superoxide dismutase, total antioxidant capacity and glutathione, and reduced mean malondialdehyde and DNA fragmentation levels, which suggested the antiapoptotic and antioxidative effects of 2-APB. |
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Note |
The technical data provided above is for reference only. |
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References: 1. 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. The Korean Journal of Physiology & Pharmacology, 2010, 14(2): 105-111. 2. Sari E, Aksit H, Erken HA, et al. Protective effect of 2-APB on testicular ischemia-reperfusion injury in rats. The Journal of Urology, 2015, 193(3): 1036-1041. |
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