DCPIB

Biological Activity

DCPIB is a volume-regulated anion channel (VRAC) blocker (IC₅₀ ~ 2 μM in rat pancreatic β-cells). Also blocks I_Cl,swell in various cardiovascular tissues (IC₅₀ = 4.1 μM in CPAE cells). Inhibits glucose-stimulated insulin secretion in intact β-cells via VSAC inhibition and indirect K_ATP channel activation. Reverses cell swelling-induced action potential duration shortening in atrial myocytes and inhibits astroglial swelling in vitro. Also activates TREK1 and TRAAK K⁺ channels and inhibits TRESK, TASK1 and TASK3 K⁺ channels at 10 μM, in vitro. Also inhibits VRAC-mediated 2'3'-cyclic-GMP-AMP (cGAMP) transport.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. Inhibition of glucose-induced electrical activity in rat pancreatic β-cells by DCPIB, a selective inhibitor of volume-sensitive anion currents.
   Best et al.
   Eur.J.Pharmacol., 2004;489:13
2. Adenosine-stimulated astroglial swelling in cat cerebral cortex in vivo with total inhibition by a non-diuretic acylaryloxyacid derivative.
   Bourke et al.
   J.Neurosurg., 1981;55:364
3. DCPIB is a novel selective blocker of I_Cl,swell and prevents swelling-induced shortening of guinea-pig atrial action potential duration.
   Decher et al.
   Br.J.Pharmacol., 2001;134:1467
4. DCPIB, an inhibitor of volume-regulated anion channels, distinctly modulates K_2P channels.
   Lv et al.
   ACS.Chem.Neurosci., 2019;
5. LRRC8A:C/E heteromeric channels are ubiquitous transporters of cGAMP.
   Lahey et al.
   Mol.Cell., 2020;80:1

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