762295-20-5Relevant articles and documents
Cardiac action of the first G protein biased small molecule apelin agonist
Read, Cai,Fitzpatrick, Christopher M.,Yang, Peiran,Kuc, Rhoda E.,Maguire, Janet J.,Glen, Robert C.,Foster, Richard E.,Davenport, Anthony P.
, p. 63 - 72 (2016)
Apelin peptide analogues displaying bias towards G protein signalling pathways have beneficial cardiovascular actions compared with the native peptide in humans in vivo. Our aim was to determine whether small molecule agonists could retain G protein bias.
An expedient synthesis of CMF-019: (s)-5-methyl-3-{1-(pentan-3-yl)-2-(thiophen-2-ylmethyl)-1h-benzo[d]imidazole-5-carboxamido}hexanoic acid, a potent apelin receptor (APJ) agonist
Trifonov, Lena,Afri, Michal,Korshin, Edward E.,Gruzman, Arie,Palczewski, Krzysztof
, p. 688 - 694 (2018/11/21)
Background: Apelin receptor (APJ) is a G protein-coupled receptor (GPCR) activated by the endogenous peptide apelin. The apelin–APJ system has emerged as an important regulator of cardiovascular homeostasis. Recently, a potent benzimidazole-derived apelin
BENZOIMIDAZOLE-CARBOXYLIC ACID AMIDE DERIVATIVES AS APJ RECEPTOR MODULATORS
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, (2014/04/17)
The present invention relates to benzoimidazole-carboxylic acid amide compounds of the formula I, in which R′, R″, R′″, R1, R2, R3, R4, R5, R6 and Z are defined as indicated below. The comp