| Bioactivity | 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]. | ||||||||||||
| Invitro | 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]. | ||||||||||||
| Name | RPR-260243 | ||||||||||||
| CAS | 668463-35-2 | ||||||||||||
| Formula | C28H25F3N2O4 | ||||||||||||
| Molar Mass | 510.50 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| 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. |
RPR-260243
CAS: 668463-35-2 F: C28H25F3N2O4 W: 510.50
RPR-260243, a potent activator of human ether-a-go-go-related gene (hERG), slows deactivation and attenuates inactivatio
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