| 2-APBantagonist of Ins(1,4,5) P3-induced Ca2+ release |
Sample solution is provided at 25 µL, 10mM.
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| Cas No. | 524-95-8 | SDF | Download SDF |
| 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 RT |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
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.
