A-887826 is a selective, orally bioavailable, and voltage-dependent Na(v1.8) channel blocker (IC50: 11 nM). It attenuates neuropathic tactile allodynia in vivo.
Ethacrynic acid, a diuretic, functions as an inhibitor of L-type voltage-dependent and store-operated calcium channels, facilitating the relaxation of airway smooth muscle (ASM) cells. It exhibits anti-inflammatory effects, notably reducing retinoid-induced ear edema in mice, and inhibits glutathione S-transferases (GSTs), making it a potent suppressor of the NF-kB signaling pathway. Additionally, ethacrynic acid modulates leukotriene formation. A variant, Ethacrynic acid D5, is distinguished by its deuterium labeling.
VBIT-3 is a voltage-dependent anion channel 1 (VDAC1) oligomerization inhibitor (Kd: 31.3 μM). VBIT-3 also is an apoptosis inhibitor, can be used for therapeutic purposes in apoptosis-associated disorders (such as neurodegenerative and cardiovascular diseases).
AKOS-22 is a potent mitochondrial protein VDAC1 (voltage-dependent anion channel 1) inhibitor (Kd=15.4 μM). AKOS-22 protects against mitochondrial dysfunction[1]. AKOS-22 interacts with VDAC1 and inhibiting both VDAC1 oligomerization and apoptosis.