BI 749327 (2361241-23-6) is a potent (IC50 = 13 nM mouse TRPC6, 19 nM human TRPC6) and selective (85-fold over TRPC3, 42-fold over TRC7) orally available blocker of TRPC6.1 It suppressed interstitial fibrosis and associated molecular signaling in mouse heart and kidney disease models.? BI 749327 reversed established pulmonary hypertension by 50% via regression of pulmonary remodeling in a mouse model.2
Lin et al. (2019) In vivo selective inhibition of TRPC6 by antagonist BI 749327 ameliorates fibrosis and dysfunction in cardiac and renal disease; Proc. Natl. Acad. Sci. USA 116 10156
Jain et al. (2021) TRPC6, a therapeutic target for pulmonary hypertension; Am. J. Physiol. Lung Cell. Mol. Physiol. 321 L1161
