RPR-260243|hERG channel activator|DC Chemicals

RPR-260243|hERG channel activator|DC Chemicals
RPR260243 was the first reported hERG channel activator.

Catlog: DC8105| Product name: RPR-260243| Cas: 668463-35-2| Other names: RPR 260243,RPR260243| Molecule Formula: C28H25F3N2O4| MW: 510.5043096. Purity: >98%

Price: 100mg: 1200 USD; 250mg: 2400 USD; 1000mg: 3800 USD

RPR260243 [(3R,4R)-4-[3-(6-methoxy-quinolin-4-yl)-3-oxo-propyl]-1-[3-(2,3,5-trifluoro-phenyl)-prop-2-yn-1-yl]-piperidine-3-carboxylic acid] was the first reported hERG channel activator. RPR260243 dramatically slows current deactivation in patch-clamp experiments, and its effect is temperature and voltage dependent. Though it is a weak inhibitor of the L-type Ca2+ channel, RPR260243 has no significant effects on the human cardiac Na+ channel or the KCNQ1/KCNE1 cardiac K+ channel, which are also linked with LQTS, thus showing high selectivity for hERG. Interestingly, RPR260243 inhibits the erg3 channel, which is in the same family as hERG, and a single S5 residue may account for this difference in pharmacology (Thr556 in hERG, Ile558 in rERG3). A Thr in this position favors agonist activity, whereas an Ile reveals a secondary blocking effect of RPR26024323. Additionally, RPR260243 enhances the delayed rectifier current in guinea pig myocytes and can, to some extent, reverse dofetilide-induced prolongation of action potential. Physiologically, it has been reported that RPR260243 can increase the T-wave amplitude, prolong the PR interval and shorten the QT interval in guinea pig hearts.

For research and scientific purpose only, not for human use.