GSK2798745

GSK2798745 is a first-in-class, potent, selective, and orally active small molecule inhibitor of the transient receptor potential vanilloid 4 (TRPV4) ion channel. It has demonstrated high affinity for human and rat TRPV4 channels with nanomolar potency (IC50s of approximately 1.8 nM for hTRPV4 and 1.6 nM for rTRPV4). The drug was developed by GSK primarily as a potential treatment for conditions involving pulmonary edema associated with heart failure and chronic cough. By blocking TRPV4-mediated calcium influx in endothelial cells, it is hypothesized to reduce pulmonary interstitial fluid accumulation and improve lung function[1][3][6][7].

Other names

UNII-63FJ7LF55OUNII63FJ7LF55OUNII 63FJ7LF55O3-[[(5S,7S)-3-[5-(2-hydroxypropan-2-yl)pyrazin-2-yl]-7-methyl-2-oxo-1-oxa-3-azaspiro[4.5]decan-7-yl]methyl]benzimidazole-5-carbonitrile1-(((5S,7S)-3-(5-(2-Hydroxypropan-2 yl)pyrazin 2 yl)-7-methyl 2 oxo 1 oxa 3 azaspiro(4.5)decan 7 yl)methyl)-1hbenzo(d)imidazole 6 carbonitrile