Cat. No. 1224
Chemical Name: 2-Aminoethoxydiphenylborane
Biological ActivityA functional and membrane permeable D-myo-inositol 1,4,5-trisphosphate (IP3) receptor antagonist (IC50 = 42 μM). Stimulates store-operated calcium (SOC) release at low concentrations (< 10 μM) and inhibits it at higher concentrations (up to 50 μM). Increases STIM-Orai channel conductance and limits ion selectivity. Modulator of TRP channels; blocks TRPC1, TRPC3, TRPC5, TRPC6, TRPV6, TRPM3, TRPM7, TRPM8 and TRPP2 and at higher concentrations stimulates TRPV1, TRPV2 and TRPV3. Also blocks specific gap channel subtypes.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Safety Data Sheet
Varnai et al (2009) STIM and Orai: the long-awaited constituents of store-operated calcium entry. TiPs 30 118. PMID: 19187978.
Togashi et al (2008) Inhibition of the transient receptor potential cation channel TRPM2 by 2-aminoethoxydiphenyl borate (2-APB). Br.J.Pharmacol. 153 1324. PMID: 18204483.
Bai et al (2006) Block of specific gap junction channel subtypes by 2-aminoethoxydiphenyl borate (2-APB). J.Pharmacol.Exp.Ther. 319 1452. PMID: 16985167.
Xu et al (2005) Block of TRPC5 channels by 2-aminoethoxydiphenyl borate: a differential, extracellular and voltafe-dependent effect. Br.J.Pharmacol. 145 405. PMID: 15806115.
Maruyama et al (1997) 2APB, 2-aminoethoxydiphenyl borate, a membrane-penetrable modulator of Ins(1,4,5)P3-induced Ca2+ release. J.Biochem. 122 498. PMID: 9348075.
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Citations are publications that use Tocris products. Selected citations for 2-APB include:
Tang et al (2015) Stimulation-evoked Ca2+ signals in astrocytic processes at hippocampal CA3-CA1 synapses of adult mice are modulated by glutamate and ATP. J Neurosci 35 3016. PMID: 25698739.
Grimes et al (2014) Cross-synaptic synchrony and transmission of signal and noise across the mouse retina. Elife 3 e03892. PMID: 25180102.
Tamura et al (2014) Both neurons and astrocytes exhibited tetrodotoxin-resistant metabotropic glutamate receptor-dependent spontaneous slow Ca2+ oscillations in striatum. PLoS One 9 e85351. PMID: 24454845.
Varadarajan et al (2013) Endoplasmic reticulum membrane reorganization is regulated by ionic homeostasis. PLoS One 8 e56603. PMID: 23457590.
Begum et al (2012) DHA inhibits ER Ca2+ release and ER stress in astrocytes following in vitro ischemia. J Neurochem 120 622. PMID: 22129278.
Lee et al (2012) The calcium-sensing receptor regulates the NLRP3 inflammasome through Ca2+ and cAMP. Nature 492 123. PMID: 23143333.
Clark et al (2009) Adenosine-evoked hyperpolarization of retinal ganglion cells is mediated by G-protein-coupled inwardly rectifying K+ and small conductance Ca2+-activated K+ channel activation. J Neurosci 29 11237. PMID: 19741130.
Dong et al (2009) P2Y receptors mediate Ca2+ signaling in duodenocytes and contribute to duodenal mucosal bicarbonate secretion. Am J Physiol Gastrointest Liver Physiol 296 G424. PMID: 19074643.
Sribnick et al (2009) Estrogen attenuates glutamate-induced cell death by inhibiting Ca2+ influx through L-type voltage-gated Ca2+ channels. Brain Res 1276 159. PMID: 19389388.
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Keywords: 2-APB, supplier, Increases, STIM-Orai, channels, conductivity, reduces, selectivity, IP3, receptor, antagonist, TRP, modulators, Store, Operated, Calcium, Channels, Ca2+, Inositol, 145-triphosphate, Receptors, Triphosphoinositol, Transient, Receptor, Potential, PIP2, Lipids, cAMP, Signaling, Signalling, TRPC1, TRPC3, TRPC5, TRPC6, TRPV6, TRPM3, TRPM7, TRPM8, TRPP2, TRPV1, TRPV2, TRPV3, Tocris Bioscience, IP3 Receptor Antagonist products
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