Uses
DCPIB is a potent, selective blocker of the volume-sensitive anion channel (VSAC) in rat pancreatic β-cells.
Definition
ChEBI: 4-[(2-butyl-6,7-dichloro-2-cyclopentyl-1-oxo-3H-inden-5-yl)oxy]butanoic acid is a member of indanones.
Biological Activity
Potent, selective blocker of the volume-sensitive anion channel (VSAC) in rat pancreatic β -cells (IC 50 ~ 2 μ M) and I Cl,swell in various cardiovascular tissues (IC 50 = 4.1 μ M in CPAE cells); blockade is voltage-independent. Displays minimal inhibition of other Cl - and K + currents (< 10% inhibition at 10 μ M). 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 .
in vivo
LDN-212854 (intracerebroventricular infusion, 1 mM, 10 μL) suppresses microglial activation and ameliorates neuronal damage in rMCAO rats[3].
| Animal Model: | Reversible middle cerebral artery occlusion (rMCAO) model[3] |
| 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. |
