646995-35-9

Usage

Biochem/physiol Actions

Cinaciguat activates sGC (soluble guanylate cyclase) independently of NO. Cinaciguat binds to sGC′s NO-sensory H-NOX domain when it is heme-depleted. Also, the compound Cinaciguat protects sGC from oxidation-induced ubiquitin-triggered degradation.

Upstream product

• 1476774-59-0 methyl 4-(((2-((4-phenethylbenzyl)oxy)phenethyl)amino)methyl)benzoate 
• 1501-26-4 methyl 4-(chlorocarbonyl)butyrate 
• 1476774-39-6 methyl 4-((5-methoxy-5-oxo-N-(2-((4-phenethylbenzyl)oxy)phenethyl)pentanamido)methyl)benzoate 
• 34224-29-8 (4-phenethylphenyl)methanol 
• 79757-91-8 1-(bromomethyl)-4-phenethylbenzene 
• 22446-37-3 methyl (2-hydroxyphenyl)acetate 
• 614-75-5 2-Hydroxyphenylacetic acid 
• 56-91-7 p-aminomethylbenzoic acid 
• 14518-67-3 methyl 4-(phenylethyl)benzoate 
• 329773-33-3 methyl 4-(((5-methoxy-5-oxopentyl)(2-((4-phenethylbenzyl)oxy)phenethyl)amino)methyl)benzoate 

Relevant academic research and scientific papers

Insights into soluble guanylyl cyclase activation derived from improved heme-mimetics

Recently, the structure of BAY 58-2667 bound to the Nostoc sp. H-NOX domain was published. On the basis of this structural information, we designed BAY 58-2667 derivatives and tested their effects on soluble guanylyl cyclase (sGC) activity. Derivative 20 activated sGC 4.8-fold more than BAY 58-2667. Co-crystallization of 20 with the Ns H-NOX domain revealed that the increased conformational distortion at the C-terminal region of αF helix containing 110-114 residues contributes to the higher activation triggered by 20.

NOVEL DERIVATIVES OF DICARBOXYLIC ACID HAVING PHARMACEUTICAL PROPERTIES

The invention relates to compounds of formulae (II), (IV), and (VI) as shown below, wherein the several variable groups are as defined in the specification and claims. Processes for making these materials, and methods for using them in the synthesis of compounds for treatment of cardiovascular disorders and fibrotic disorders are also disclosed.