Cas No.: | 2747162-85-0 |
Chemical Name: | MCUF-651 |
Synonyms: | MCUF651 |
SMILES: | O=C(C1CN(CCN(C)C)CCC1)NC2=NC3=C(F)C=C(F)C=C3S2 |
Formula: | C17H22F2N4Os |
M.Wt: | 368.447 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Publication: | 1. S Jeson Sangaralingham, et al. Proc Natl Acad Sci U S A. 2021 Dec 28;118(52):e2109386118 |
Description: | 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. |
References: | 1. S Jeson Sangaralingham, et al. Proc Natl Acad Sci U S A. 2021 Dec 28;118(52):e2109386118 |