HS-142-1   Click here for help

GtoPdb Ligand ID: 4952

Synonyms: HS142-1
Comment: HS-142-1, a novel nonpeptide (polysaccharide) atrial natriuretic peptide (ANP) antagonist which specifically inhibits natriuretic peptide-induced vasorelaxation through the blockade of guanylyl cyclase-linked natriuretic peptide receptors [1]. It was purified from the fermentation broth of Aureobasidium pullulans var. melanigenum [3]. The compound consists of glucose and caproyl subunits. Hexaosyl fragment O-(3-O-caproyl-beta-D-glucopyranosyl)-(1-->6)-[O-(beta-D- glucopyranosyl)-(1-->6)-O-(3-O-caproyl-beta-D-glucopyranosyl)-(1--> 6)]2-D-glucopyranose, is among the major components of the molecule and ithis has been used as the basis for synthesising synthetic analogues of the polysaccharide.
Bioactivity Comments
HS-142-1 inhibits [125I]-rANP binding to ANP receptor in rabbit kidney cortex membranes with an IC50 of 0.3µg/ml [2].
Selectivity at catalytic receptors
Key to terms and symbols Click column headers to sort
Target Sp. Type Action Value Parameter Concentration range (M) Reference
Guanylyl cyclase-A Hs Antagonist Antagonist - - - 2
[2]
Guanylyl cyclase-B Hs Antagonist Antagonist - - - 2
[2]