- Herrington, J. et al. (2011) Mol. Pharmacol. 80, 959.
- Alomone Labs RY796 inhibits KV2.1 channels expressed in Xenopus oocytes.A. Time course of KV2.1 current amplitude, elicited by 100 ms voltage step from holding potential of -100 mV to +50 mV,delivered every 10 seconds. Application of 1 and 10 µM RY796 (#R-160) inhibits the KV2.1 current in a reversible manner (indicated by the horizontal bar). B. Representative current traces before and during application of 1 and 10 µM RY796 as indicated.
KV channels are voltage-gated potassium channels that open in response to membrane depolarization thus serving as key elements after cell repolarization. KV channels regulate numerous physiological processes. KV2 channels are widely expressed in the CNS, pancreas and smooth muscle.
RY796 is a synthetic blocker of the KV2.1 and KV2.2 channels. It has an effective concentration of 0.1-10 µM and an IC50 of 0.09 µM and 0.25 µM for the KV2.1 and KV2.2 channels respectively. RY796 has greater selectivity for KV2 channels over other KV channels out of 1894 compounds in a study conducted by Herrington, J. et al. In addition, RY796 does not affect other ion channels such as sodium and calcium.
RY796 blocks the KV channel in a use and dose dependent manner1. In an experiment examining the role of KV channels in the regulation of insulin and somatostatin release from pancreatic islets, RY796 caused an increase of GSIS (glucose stimulated insulin secretion) in vitro however not producing the same effect in live mice. RY796 was also found to increase glucose stimulated somatostatin release from pancreatic δ-cells2.
RY796 (#R-160) is a highly pure, synthetic, and biologically active compound.