RPR-260243

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.

Product Specifications

CAS Number

[668463-35-2]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Potassium Channel

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel

Applications

COVID-19-immunoregulation

Field of Research

Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/RPR-260243.html

Purity

99.91

Solubility

DMSO : 10 mg/mL (ultrasonic)

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

Molecular Formula

C28H25F3N2O4

Molecular Weight

510.50

Precautions

H302, H315, H319, H335

References & Citations

[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.