2-APBCat. No. 1224 |
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Chemical Name: 2-Aminoethoxydiphenylborane |
Biological Activity
A 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.Technical Data
M.Wt:The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Certificate of Analysis / Safety Data Sheet
References
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.
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.
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.
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.
Varnai et al (2009) STIM and Orai: the long-awaited constituents of store-operated calcium entry. TiPs 30 118. PMID: 19187978.
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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
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