BI-749327

BI-749327 is an inhibitor of transient receptor potential canonical 6 (TRPC6; IC₅₀ = 13 nM for the mouse channel).¹ It is selective for TRPC6 over TRPC3 and TRPC7 (IC₅₀s = 1,100 and 550 nM, respectively, for the mouse channels). BI-749327 (100, 250, and 500 nM) inhibits TRPC6-mediated reporter gene expression in HEK293T cells expressing mouse TRPC6. In vivo, BI-749327 (30 mg/kg) decreases myocardial interstitial fibrosis in a mouse model of hypertrophic cardiomyopathy induced by transaortic constriction. It reduces unilateral ureteral obstruction-induced renal fibrosis in mice. BI-749327 (30 mg/kg) also increases survival, decreases myocardial fibrosis, and improves grip strength in a mouse model of Duchenne muscular dystrophy (DMD).²

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1. Lin, B.L., Matera, D., Doerner, J.F., et al. 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(20), 10156-10161 (2019).

2. Lin, B.L., Shin, J.Y., Jeffreys, W.P., et al. Pharmacological TRPC6 inhibition improves survival and muscle function in mice with Duchenne muscular dystrophy. JCI Insight 7(19), e158906 (2022).