| Bioactivity | DCPIB is a selective, reversible and potent inhibitor of volume-regulated anion channels (VRAC). DCPIB voltage-dependently activates potassium channels TREK1 and TRAAK, and inhibits TRESK, TASK1 and TASK3 (IC50s: 0.14, 0.95, 50.72 μM, respectively). DCPIB is also a selective blocker of swelling-induced chloride current (ICl,swell), with an IC50 of 4.1 μM. DCPIB is a useful tool for investigating structure-function studies of K2P channels[1][2]. | ||||||||||||
| Target | IC50：0.14 μM (TRESK), 0.95 μM (TASK1), 50.72 μM (TASK3), 4.1 μM (ICl,swell, CPAE cells) | ||||||||||||
| Invitro | DCPIB (10 μM) activates TREK1 and enhances TRAAK currents in COS-7 cells[1].DCPIB (10 μM) prominently and reversibly suppresses TRESK currents in COS-7 cells, with an IC50 of 0.14 μM[1].DCPIB (10 μM) displays selectivity for ICl,swell and has no significant inhibitory effects on ICl,Ca in CPAE cells[2].DCPIB (10 μM, 5 min) has no effect on attenuate subsequent swelling in cardiomyocytes[2].DCPIB (10 μM, 3 h) inhibits LPS-induced MAPK activation in BV2 cells[3]. Immunofluorescence[3] Cell Line: | ||||||||||||
| In Vivo | LDN-212854 (intracerebroventricular infusion, 1 mM, 10 μL) suppresses microglial activation and ameliorates neuronal damage in rMCAO rats[3]. Animal Model: | ||||||||||||
| Name | DCPIB | ||||||||||||
| CAS | 82749-70-0 | ||||||||||||
| Formula | C22H28Cl2O4 | ||||||||||||
| Molar Mass | 427.36 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Lv J, et al. DCPIB, an Inhibitor of Volume-Regulated Anion Channels, Distinctly Modulates K2P Channels. ACS Chem Neurosci. 2019 Apr 17. [2]. Decher N, et al. DCPIB is a novel selective blocker of I(Cl,swell) and prevents swelling-induced shortening of guinea-pig atrial action potential duration. Br J Pharmacol. 2001 Dec;134(7):1467-79. [3]. Qingdong Han, et al. DCPIB, a potent volume-regulated anion channel antagonist, attenuates microglia-mediated inflammatory response and neuronal injury following focal cerebral ischemia. Brain Res. 2014 Jan 13;1542:176-85. |