For research use only. Not for therapeutic Use.
RPR-260243, a potent activator of human ether-a-go-go-related gene (hERG), slows deactivation and attenuates inactivation of hERG1 channels. RPR260243-modified HERG currents are inhibited by Dofetilide (IC50=58 nM). RPR260243 displays no activator-like effects on other voltage-dependent ion channels, including the closely related ERG3 K+ channel[1][2]. RPR-260243 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
RPR-260243 enhances the delayed rectifier current in guinea pig myocytes but, when administered alone, has little effect on action potential parameters in these cells[2].
| Catalog Number | I004516 |
| CAS Number | 668463-35-2 |
| Synonyms | (3R,4R)-4-[3-(6-methoxyquinolin-4-yl)-3-oxopropyl]-1-[3-(2,3,5-trifluorophenyl)prop-2-ynyl]piperidine-3-carboxylic acid |
| Molecular Formula | C28H25F3N2O4 |
| Purity | ≥95% |
| InChI | InChI=1S/C28H25F3N2O4/c1-37-20-5-6-25-22(15-20)21(8-10-32-25)26(34)7-4-17-9-12-33(16-23(17)28(35)36)11-2-3-18-13-19(29)14-24(30)27(18)31/h5-6,8,10,13-15,17,23H,4,7,9,11-12,16H2,1H3,(H,35,36)/t17-,23+/m1/s1 |
| InChIKey | VWNMWKSURFWKAL-HXOBKFHXSA-N |
| SMILES | COC1=CC2=C(C=CN=C2C=C1)C(=O)CCC3CCN(CC3C(=O)O)CC#CC4=C(C(=CC(=C4)F)F)F |
| Reference | [1]. Wu W, et al. Concatenated hERG1 tetramers reveal stoichiometry of altered channel gating by RPR-260243. Mol Pharmacol. 2015;87(3):401-409. [2]. Kang J, et al. Discovery of a small molecule activator of the human ether-a-go-go-related gene (HERG) cardiac K+ channel. Mol Pharmacol. 2005;67(3):827-836. |
