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VU0493206
- Development stage
- Preclinical
- Lead developer
- Vanderbilt University
- Modality
- Small Molecules
01
Overview
VU0493206 is a small-molecule activator (potentiator) of heteromeric Kir4.1/Kir5.1 (KCNJ10/KCNJ16) inwardly rectifying potassium channels. Discovered through high-throughput screening of over 80,000 compounds, VU0493206 selectively activates Kir4.1/Kir5.1-mediated currents and hyperpolarizes the membrane potential of renal epithelial cells. It has demonstrated selectivity for Kir4.1/Kir5.1 over other members of the Kir channel family. VU0493206 is being investigated for its potential to rescue loss-of-function mutations in KCNJ10 and KCNJ16, which are associated with SeSAME/EAST syndrome and other renal tubulopathies.
02
Targets
KCNJ10 (Kir4.1)Potassium inwardly rectifying channel subfamily J member 16
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