MCUF-651 (MCUF651) is a small molecule guanylyl cyclase A receptor (GC-A) positive allosteric modulator (PAM), potentiate ANP-mediated cGMP with EC50 of 0.45 uM (Emax=82%) in HEK293 GC-A cells.MCUF-651 enhanced ANP-mediated cGMP generation in human cardiac, renal, and fat cells and inhibited cardiomyocyte hypertrophy in vitro.MCUF-651 binds to GC-A (Kd=397 nM) and selectively enhances the binding of ANP to GC-A ( MCUF-651+ANP, Kd=0.06 nM).MCUF-651 is orally bioavailable in mice and enhances the ability of endogenous ANP and BNP to generate GC-A-mediated cGMP ex vivo.
Cat.No
DC70592
Name
MCUF-651
Chemical Properties
CAS
2747162-85-0
Formula
C17H22F2N4OS
MW
368.447
Storage
2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
References
1. S Jeson Sangaralingham, et al. Proc Natl Acad Sci U S A. 2021 Dec 28;118(52):e2109386118
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