DCPIB 是选择性可逆体积调节性阴离子通道抑制剂，抑制肿胀激活氯电流，在 CPAE 细胞中，IC50值为 4.1 μM。它能够电压依赖性激活钾离子通道 TREK1 和 TRAAK，抑制 TRESK、TASK1 和 TASK3的IC50值分别为 0.14、0.95 和 50.72 μM。

DCPIB, a known specific and potent inhibitor of volume-regulated anion channels (VRAC),DCPIB displayed superior selectivity toward TRESK with an IC50 of 0.14 μM, demonstrating at least 100-fold higher affinity over TREK1/TRAAK channels.

DCPIB, a known specific and potent inhibitor of volume-regulated anion channels (VRAC), has been reported to activate TREK1 and TREK2 in astrocytes and in vitro recently.?In the present study, we demonstrated DCPIB also voltage dependently activated TRAAK besides TREK1/TREK2, showing DCPIB activated all TREK subfamily members.?In contrast, the compound potently inhibited several other K2P channels with no voltage dependence, including TRESK, TASK1, and TASK3.?DCPIB displayed superior selectivity toward TRESK with an IC50 of 0.14 μM, demonstrating at least 100-fold higher affinity over TREK1/TRAAK channels.?Furthermore, the impaired ion selectivity filter region greatly impaired the activating effect of DCPIB on TREK1 but not the inhibitory effect of DCPIB on TRESK.?This indicates distinct molecular determinants underlying the effect of DCPIB on TREK1 or TRESK channels.?DCPIB played diverse effects on K2P channels and could be a useful tool for further investigating structure-function studies of K2P channels.

82749-70-0

C22H28Cl2O4

427.36

DMSO:125 mg/mL (292.49 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years