Name | DCPIB |
Description | 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. |
In vitro | 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.
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Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | DMSO : 125 mg/mL (292.49 mM)
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Keywords | Cl-Channels | Chloride Channel | cardiomyocytes | ischemia | COS-7 | KcsA | Potassium Channel | CPAE cell | Inhibitor | DCPIB | inhibit | swelling | rMCAO |
Inhibitors Related | Minoxidil sulfate | Quinine | (±)-Naringenin | Tolbutamide | Tetraethylammonium bromide | Halothane | Butamben | Tetraethylammonium chloride | Cloperastine hydrochloride | Fenamic acid | 2,2,2-Trichloroethanol | Indapamide |
Related Compound Libraries | 经典已知活性库 | 疼痛相关化合物库 | 膜蛋白靶向化合物库 | 抑制剂库 | NO PAINS 化合物库 | 已知活性化合物库 | 钾通道分子库 | 共价抑制剂库 | 离子通道库 | 抗癌化合物库 |