DCPIB

SKU: orb1219386

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. 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.

Key Properties

• CAS Number: 82749-70-0
• MW: 427.36
• Purity: >98% (HPLC)
• Formula: C₂₂H₂₈Cl₂O₄
• SMILES: O=C(O)CCCOC1=CC2=C(C(C(C3CCCC3)(CCCC)C2)=O)C(Cl)=C1Cl
• Target: Chloride Channel
• Solubility: DMSO:125 mg/mL (292.49 mM)

Bioactivity

• In Vivo:
  Animal model: Reversible middle cerebral artery occlusion (rMCAO) model. Dosage: 1 mM, 10 μL. Administration: Administered manually for 20s by intracerebroventricular infusion. Result: Diminished Pyramidal neurons injury induced by rMCAO in the CA1 region.
• In Vitro:
  Immunofluorescence Cell line: BV2 cells. Concentration: 10 μM. Incubation time: 3 h. Result: Significantly decreased Ki67 positive staining microglia and pro-inflammatory cytokine (TNF-α, IL-1β) secretion. Western blot analysis. Cell line: BV2 cells. Concentration: 10 μM. Incubation time: 3 h. Result: Inhibited migratory potential of transient OGD (Oxygen-glucose deprivation) exposed BV2 cells.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

Chloride Channel