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SAR7334 is a transient receptor potential canonical 6 (TRPC6) channel blocker (IC50 = 7.9 nM).1 It is selective for TRPC6 over TRPC4 and TRPC5 (IC50s = 282 and 226 nM, respectively). SAR7334 (0.2-1 μM) blocks TRPC6-dependent hypoxia-induced vasoconstriction in isolated perfused and ventilated mouse lung. It also inhibits oxidative stress-induced apoptosis and increases autophagic flux in primary mouse renal proximal tubule cells.2
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1. Discovery and pharmacological characterization of a novel potent inhibitor of diacylglycerol-
2. Transient receptor potential channel 6 knockdown prevents apoptosis of renal tubular epithelial cells upon oxidative stress via autophagy activation. Cell Death Dis. 9(10), 1015 (2018).