MCUF-651

A GC-A positive allosteric modulator, induces the production of cGMP in the presence (EC50 = 0.45 µM) but not the absence of ANP in HEK293 cells expressing human GC-A, selective for GC-A over GC-B in HEK293 cells expressing the human receptors at 10 µM, binds to the GC-A extracellular domain (Kd = 397 nM) and enhances the binding of ANP to the GC-A extracellular domain in cell-free assays, enhances ANP-induced production of cGMP in primary human renal proximal tubular cells, visceral adipocytes, and cardiomyocytes from 1-10 µM, inhibits TGF-ß1-induced hypertrophy of primary human cardiomyocytes in combination with ANP, induces cGMP production in GC-A-expressing HEK293 cells incubated with plasma isolated from patients with hypertension or heart failure. Formulation: A solid. InChI: InChI=1S/C17H22F2N4OS/c1-22(2)6-7-23-5-3-4-11(10-23)16(24)21-17-20-15-13(19)8-12(18)9-14(15)25-17/h8-9,11H,3-7,10H2,1-2H3,(H,20,21,24). InChIKey: NOPAIELWJAFUCL-UHFFFAOYSA-N. SMILES: CN(CCN1CCCC(C(NC2=NC3=C(C=C(C=C3F)F)S2)=O)C1)C