RPR-260243
Modify Date: 2026-07-17 07:30:25
RPR-260243 structure
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Common Name | RPR-260243 | ||
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| CAS Number | 668463-35-2 | Molecular Weight | 510.50400 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C28H25F3N2O4 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of RPR-260243RPR-260243 is a novel activator of HERG; modifies HERG currents inhibited by dofetilide (IC50 = 58 nM); little effect on HERG current amplitude and no significant effects on steady-state activation parameters or on channel inactivation processes.IC50 value: Target: HERG activatorRPR260243 displayed no activator-like effects on other voltage-dependent ion channels, including the closely related erg3 K+ channel. RPR260243 enhanced the delayed rectifier current in guinea pig myocytes but, when administered alone, had little effect on action potential parameters in these cells. However, RPR260243 completely reversed the action potential-prolonging effects of dofetilide in this preparation. Using the Langendorff heart method, we found that 5 μM RPR260243 increased T-wave amplitude, prolonged the PR interval, and shortened the QT interval. We believe RPR260243 represents the first known HERG channel activator and that the drug works primarily by inhibiting channel closure, leading to a persistent HERG channel current upon repolarization. |
| Name | (3R,4R)-4-[3-(6-methoxyquinolin-4-yl)-3-oxopropyl]-1-[3-(2,3,5-trifluorophenyl)prop-2-ynyl]piperidine-3-carboxylic acid |
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| Synonym | More Synonyms |
| Description | RPR-260243 is a novel activator of HERG; modifies HERG currents inhibited by dofetilide (IC50 = 58 nM); little effect on HERG current amplitude and no significant effects on steady-state activation parameters or on channel inactivation processes.IC50 value: Target: HERG activatorRPR260243 displayed no activator-like effects on other voltage-dependent ion channels, including the closely related erg3 K+ channel. RPR260243 enhanced the delayed rectifier current in guinea pig myocytes but, when administered alone, had little effect on action potential parameters in these cells. However, RPR260243 completely reversed the action potential-prolonging effects of dofetilide in this preparation. Using the Langendorff heart method, we found that 5 μM RPR260243 increased T-wave amplitude, prolonged the PR interval, and shortened the QT interval. We believe RPR260243 represents the first known HERG channel activator and that the drug works primarily by inhibiting channel closure, leading to a persistent HERG channel current upon repolarization. |
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| Related Catalog | |
| References |
| Molecular Formula | C28H25F3N2O4 |
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| Molecular Weight | 510.50400 |
| Exact Mass | 510.17700 |
| PSA | 79.73000 |
| LogP | 4.63590 |
| InChIKey | VWNMWKSURFWKAL-HXOBKFHXSA-N |
| SMILES | COc1ccc2nccc(C(=O)CCC3CCN(CC#Cc4cc(F)cc(F)c4F)CC3C(=O)O)c2c1 |
| Storage condition | 2-8℃ |
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Name: Activation of human ERG1 V549A mutant expressed in Xenopus laevis oocytes assessed as...
Source: ChEMBL
Target: Potassium voltage-gated channel subfamily H member 2
External Id: CHEMBL933614
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Name: Activation of human ERG1 Y667A mutant expressed in Xenopus laevis oocytes assessed as...
Source: ChEMBL
Target: Potassium voltage-gated channel subfamily H member 2
External Id: CHEMBL933613
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|
Name: Primary qHTS assay for small molecule inhibitors of Inositol hexaphosphate kinase 1 (...
Source: NCGC
External Id: IP6K1-p1
|
|
Name: Activation of human ERG1 F557L mutant expressed in Xenopus laevis oocytes assessed as...
Source: ChEMBL
Target: Potassium voltage-gated channel subfamily H member 2
External Id: CHEMBL933617
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Name: Activation of human ERG1 L550A mutant expressed in Xenopus laevis oocytes assessed as...
Source: ChEMBL
Target: Potassium voltage-gated channel subfamily H member 2
External Id: CHEMBL933615
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|
Name: Activation of human ERG1 V659A mutant expressed in Xenopus laevis oocytes assessed as...
Source: ChEMBL
Target: Potassium voltage-gated channel subfamily H member 2
External Id: CHEMBL933610
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Name: Activation of human ERG1 N658A mutant expressed in Xenopus laevis oocytes assessed as...
Source: ChEMBL
Target: Potassium voltage-gated channel subfamily H member 2
External Id: CHEMBL925855
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|
Name: Activation of human ERG1 L666A mutant expressed in Xenopus laevis oocytes assessed as...
Source: ChEMBL
Target: Potassium voltage-gated channel subfamily H member 2
External Id: CHEMBL933612
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|
Name: Activation of human ERG1 I662A mutant expressed in Xenopus laevis oocytes assessed as...
Source: ChEMBL
Target: Potassium voltage-gated channel subfamily H member 2
External Id: CHEMBL933611
|
|
Name: Cytochrome P450 family 3 subfamily A member 4 (CYP3A4) small molecule antagonists: lu...
Source: NCGC
External Id: CYP3A4437
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| qcr-62 |
| RPR-260243 |