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| Targets |
RPR260243 targets the voltage-gated potassium channel Kv11.1 (KCNH2), also known as the hERG channel. It acts as an activator of this channel. Some sources also describe it as a selective inhibitor of HDAC6. The primary mechanism of action is modulation of hERG channel function.
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| ln Vitro |
When introduced alone, RPR-260243 improves delayed rectifier currents in guinea pig myocytes but has minimal influence on action potential characteristics in these cells [2].
RPR260243 is an activator of the hERG potassium channel, with an IC50 of 58 nM for modifying hERG currents inhibited by dofetilide. It has little effect on hERG current amplitude and no significant effects on steady-state activation parameters or on channel inactivation processes. This demonstrates its specific modulatory effects on hERG channel function. |
| ln Vivo |
Specific in vivo data for RPR260243 is not detailed in the available literature. As an hERG channel activator, it has been studied for its potential to modulate cardiac repolarization and treat arrhythmias. It has also shown promise in preclinical studies for its ability to modulate the acetylation of tubulin via HDAC6 inhibition.
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| Enzyme Assay |
The in vitro activity of RPR260243 is assessed using electrophysiological techniques. In these assays, cells expressing the hERG channel (typically HEK-293 cells) are subjected to patch-clamp recording. The compound is applied at various concentrations, and its effect on hERG currents is measured. The IC50 of 58 nM is determined from these assays.
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| Cell Assay |
Cell-based assays are used to evaluate RPR260243's activity on hERG channels. Cells expressing hERG are treated with the compound, and the hERG current is measured using whole-cell patch-clamp electrophysiology. The compound's ability to modify hERG currents inhibited by dofetilide is assessed. For HDAC6 inhibition, the acetylation of tubulin can be measured by Western blot.
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| Animal Protocol |
RPR260243 has been evaluated in preclinical studies for its potential to modulate cardiac repolarization and treat arrhythmias. In these studies, the compound is typically administered to animal models, and its effects on cardiac electrophysiology and other endpoints are assessed. However, specific protocols are not detailed in the available literature.
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| ADME/Pharmacokinetics |
RPR260243 has a molecular weight of 510.50 and a molecular formula of C28H25F3N2O4. It is soluble in DMSO. Purity is typically ≥98% by HPLC. The compound is a selective activator of the hERG potassium channel and is also described as a selective HDAC6 inhibitor.
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| Toxicity/Toxicokinetics |
RPR260243 is a research compound and its full toxicological profile is not detailed in the available literature. As a modulator of hERG channels, it has the potential to affect cardiac repolarization and could have proarrhythmic effects. Its safety profile would be evaluated in preclinical toxicology studies for its development as a therapeutic agent.
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| References | |
| Additional Infomation |
RPR260243 (CAS#: 668463-35-2) is a selective activator of the hERG cardiac K+ channel, with an IC50 of 58 nM for modifying dofetilide-inhibited hERG currents. It has little effect on hERG current amplitude and no significant effects on channel activation or inactivation. RPR260243 is also described as a selective HDAC6 inhibitor. It is a research tool for studying hERG channel function and cardiac electrophysiology.
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| Molecular Formula |
C28H25F3N2O4
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|---|---|
| Molecular Weight |
510.51
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| Exact Mass |
510.177
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| CAS # |
668463-35-2
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| PubChem CID |
11466357
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| Appearance |
Light yellow to light brown solid powder
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| LogP |
4.635
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
37
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| Complexity |
876
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| Defined Atom Stereocenter Count |
2
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| SMILES |
COC1=CC2=C(C=CN=C2C=C1)C(=O)CC[C@@H]3CCN(C[C@@H]3C(=O)O)CC#CC4=C(C(=CC(=C4)F)F)F
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| InChi Key |
VWNMWKSURFWKAL-HXOBKFHXSA-N
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| InChi Code |
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
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| Chemical 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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| Synonyms |
RPR-260243; RPR 260243; RPR260243
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~10 mg/mL (~19.59 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (1.96 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1 mg/mL (1.96 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1 mg/mL (1.96 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9588 mL | 9.7941 mL | 19.5883 mL | |
| 5 mM | 0.3918 mL | 1.9588 mL | 3.9177 mL | |
| 10 mM | 0.1959 mL | 0.9794 mL | 1.9588 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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