| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Other Sizes |
| Targets |
RL648_81 targets KCNQ2/3 (Kv7.2/7.3) potassium channels, which are voltage-gated potassium channels that play a critical role in regulating neuronal excitability. As a selective activator, RL648_81 shifts the voltage dependence of channel activation to more hyperpolarized potentials, increasing the probability of channel opening at resting membrane potentials. This enhances the M-current, reducing neuronal hyperexcitability. It has no effect on KCNQ4 or KCNQ5 channels.
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| ln Vitro |
In vitro, RL648_81 is a potent and selective activator of KCNQ2/3 channels with an EC50 of 190 nM. It robustly shifts the V1/2 of KCNQ2/3 channels towards hyperpolarized potentials. It does not shift the V1/2 of either KCNQ4 or KCNQ5. Its activity is confirmed in electrophysiological assays using cells expressing KCNQ2/3 channels.
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| ln Vivo |
In vivo, RL648_81 has potential for neurologic disorders associated with neuronal hyperexcitability. Its ability to activate KCNQ2/3 channels and reduce neuronal excitability suggests potential therapeutic applications in epilepsy, neuropathic pain, and other hyperexcitability disorders. However, specific in vivo efficacy data are limited.
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| Enzyme Assay |
Cell-free assays for RL648_81 are not standard because it targets ion channels. Its activity is assessed using electrophysiological techniques such as patch-clamp on cells expressing KCNQ2/3 channels. The compound's ability to shift the voltage dependence of channel activation is measured. Its molecular weight (371.34) and formula (C17H17F4N3O2) are confirmed by mass spectrometry.
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| Cell Assay |
Cellular assays for RL648_81 are performed using cell lines expressing KCNQ2/3 channels, such as CHO or HEK293 cells. Cells are treated with varying concentrations of RL648_81, and potassium currents are measured using patch-clamp electrophysiology. The EC50 for channel activation and the shift in V1/2 are determined. Cell viability is evaluated using standard assays.
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| Animal Protocol |
In vivo animal experiments for RL648_81 are not extensively documented. To evaluate its efficacy in neurological disorders, animal models of epilepsy, neuropathic pain, or anxiety could be used. Animals would be administered RL648_81 via oral or intraperitoneal injection, and behavioral and electrophysiological endpoints would be assessed.
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| ADME/Pharmacokinetics |
RL648_81 has a molecular weight of 371.34 g/mol and a molecular formula of C17H17F4N3O2. It has a purity of 98%. It is soluble in DMSO. It should be stored under recommended conditions. Its chemical name is ethyl N-[2-amino-3-fluoro-4-[[4-(trifluoromethyl)phenyl]methylamino]phenyl]carbamate.
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| Toxicity/Toxicokinetics |
The toxicological profile of RL648_81 has not been extensively characterized. As a research compound, it is generally considered safe at the concentrations used in studies. No significant toxicity has been reported. Comprehensive toxicology studies are lacking. It is not an approved drug and is intended for research use only.
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| References | |
| Additional Infomation |
RL648_81 is a selective activator of KCNQ2/3 potassium channels with an EC50 of 190 nM. It has potential for research in neurological disorders associated with neuronal hyperexcitability. It robustly shifts the V1/2 of KCNQ2/3 channels towards hyperpolarized potentials and has no effect on KCNQ4 or KCNQ5. It is a research compound and is not approved for clinical use.
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| Molecular Formula |
C17H17F4N3O2
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|---|---|
| Molecular Weight |
371.329397916794
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| Exact Mass |
371.125
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| CAS # |
1919050-87-5
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| PubChem CID |
124203920
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
412.8±45.0 °C at 760 mmHg
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| Flash Point |
203.4±28.7 °C
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| Vapour Pressure |
0.0±1.0 mmHg at 25°C
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| Index of Refraction |
1.595
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| LogP |
1.97
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
26
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| Complexity |
456
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCOC(=O)NC1=C(C(=C(C=C1)NCC2=CC=C(C=C2)C(F)(F)F)F)N
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| InChi Key |
MVSMZQRRMPUGHI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H17F4N3O2/c1-2-26-16(25)24-13-8-7-12(14(18)15(13)22)23-9-10-3-5-11(6-4-10)17(19,20)21/h3-8,23H,2,9,22H2,1H3,(H,24,25)
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| Chemical Name |
ethyl N-[2-amino-3-fluoro-4-[[4-(trifluoromethyl)phenyl]methylamino]phenyl]carbamate
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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 : ~100 mg/mL (~269.30 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.73 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6930 mL | 13.4651 mL | 26.9302 mL | |
| 5 mM | 0.5386 mL | 2.6930 mL | 5.3860 mL | |
| 10 mM | 0.2693 mL | 1.3465 mL | 2.6930 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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