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668463-35-2

668463-35-2 Structure

668463-35-2 Structure
IdentificationBack Directory
[Name]

RPR-260243
[CAS]

668463-35-2
[Synonyms]

100866
CS-2094
RPR-260243
RPR 260243;RPR260243
(3R,4R)-4-[3-(6-Methoxyquinolin-4-yl)-3-oxo-propyl]-1-[3-(2,3,5-trifluoro-phenyl)-prop-2-ynyl]
(3R,4R)-4-[3-(6-Methoxyquinolin-4-yl)-3-oxo-propyl]-1-[3-(2,3,5-trifluoro-phenyl)-prop-2-ynyl]-piperidine-3-carboxylic acid
3-Piperidinecarboxylic acid, 4-[3-(6-methoxy-4-quinolinyl)-3-oxopropyl]-1-[3-(2,3,5-trifluorophenyl)-2-propyn-1-yl]-, (3R,4R)-
[Molecular Formula]

C28H25F3N2O4
[MDL Number]

MFCD23136021
[MOL File]

668463-35-2.mol
[Molecular Weight]

510.5
Chemical PropertiesBack Directory
[Boiling point ]

668.0±55.0 °C(Predicted)
[density ]

1.38±0.1 g/cm3(Predicted)
[storage temp. ]

Store at 2-8°C
[solubility ]

DMSO: 10 mg/mL (19.59 mM)
[form ]

Solid
[pka]

3.71±0.40(Predicted)
[color ]

Light yellow to light brown
Hazard InformationBack Directory
[Uses]

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.
[References]

[1] Wu W, et al. Concatenated hERG1 tetramers reveal stoichiometry of altered channel gating by RPR-260243. Mol Pharmacol. 2015;87(3):401-409. DOI:10.1124/mol.114.096693
[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. DOI:10.1124/mol.104.006577
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