Formulation: A solid
Formal Name: [4-(6-amino-3-pyridazinyl)-1-piperidinyl][4-[4-(trifluoromethyl)phenoxy]phenyl]-methanone
Purity: ≥98%
Formula Markup: C23H21F3N4O2
Formula Weight: 442,4
Shelf life (days): 1460
CAS Number: 2361241-23-6
Notes: BI-749327 is an inhibitor of transient receptor potential canonical 6 (TRPC6; IC50 = 13 nM for the mouse channel).{72417} 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).{72418}
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