RPR-260243|hERG channel activator|DC Chemicals

Cas No.:	668463-35-2
Chemical Name:	(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
Synonyms:	RPR 260243,RPR260243
SMILES:	O=C([C@H]1CN(CC#CC2=CC(F)=CC(F)=C2F)CC[C@H]1CCC(C3=CC=NC4=CC=C(OC)C=C34)=O)O
Formula:	C₂₈H₂₅F₃N₂O₄
M.Wt:	510.5043096
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

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 the detailed information of RPR-260243, the solubility of RPR-260243 in water, the solubility of RPR-260243 in DMSO, the solubility of RPR-260243 in PBS buffer, the animal experiment (test) of RPR-260243, the cell expriment (test) of RPR-260243, the in vivo, in vitro and clinical trial test of RPR-260243, the EC50, IC50,and affinity,of RPR-260243, For the detailed information of RPR-260243, the solubility of RPR-260243 in water, the solubility of RPR-260243 in DMSO, the solubility of RPR-260243 in PBS buffer, the animal experiment (test) of RPR-260243, the cell expriment (test) of RPR-260243, the in vivo, in vitro and clinical trial test of RPR-260243, the EC50, IC50,and affinity,of RPR-260243, Please contact DC Chemicals.

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2018-0101

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