BI-749327

BI-749327 is an inhibitor of transient receptor potential canonical 6 (TRPC6, IC50 = 13 nM for the mouse channel). 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).Formal Name: [4-(6-amino-3-pyridazinyl)-1-piperidinyl][4-[4-(trifluoromethyl)phenoxy]phenyl]-methanone. CAS Number: 2361241-23-6. Molecular Formula: C23H21F3N4O2. Formula Weight: 442.4. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: Acetonitrile: Slightly Soluble: 0.1-1 mg/ml, DMSO: Sparingly Soluble: 1-10 mg/ml. SMILES: O=C(N1CCC(CC1)C2=CC=C(N)N=N2)C3=CC=C(C=C3)OC4=CC=C(C(F)(F)F)C=C4. InChi Code: InChI=1S/C23H21F3N4O2/c24-23(25,26)17-3-7-19(8-4-17)32-18-5-1-16(2-6-18)22(31)30-13-11-15(12-14-30)20-9-10-21(27)29-28-20/h1-10,15H,11-14H2,(H2,27,29). InChi Key: RGYMFGHHIDRCBN-UHFFFAOYSA-N.