| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
DMP-543 targets KV7 (KCNQ) potassium channels. By blocking these channels, it enhances neuronal excitability and promotes neurotransmitter release. It specifically enhances the release of acetylcholine, dopamine, and glutamate. This mechanism is relevant to cholinergic signaling and cognition.
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|---|---|
| ln Vitro |
DMP-543, with an EC50 of 700 nM, increases the release of [3H]ACh in rat brain slices [2].
In vitro, DMP-543 enhances K+-stimulated [³H]-ACh release from rat hippocampal slices with an EC50 of 700 nM. It also increases the release of dopamine and glutamate with EC50 values of 0.25 and 0.22 μM, respectively. These effects are consistent with its role as a neurotransmitter release enhancer. |
| ln Vivo |
In vivo, DMP-543 is orally active. Its ability to enhance neurotransmitter release and its anticonvulsant effects have been observed in animal models. However, specific in vivo efficacy data are not detailed in the available sources.
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| Enzyme Assay |
In vitro receptor/enzyme binding assays are not applicable for DMP-543, as its primary target is the KV7 potassium channel. Its activity is assessed in functional assays measuring ion flux through the channel. Patch-clamp electrophysiology is used to directly measure the compound's inhibition of potassium currents in cells expressing KV7 channels.
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| Cell Assay |
In vitro cellular assays for DMP-543 involve measuring its effect on neurotransmitter release. Rat hippocampal slices are pre-loaded with [³H]-choline, which is taken up and converted to [³H]-ACh. The slices are then stimulated with high potassium in the presence of the compound, and the amount of [³H]-ACh released into the medium is measured by scintillation counting. This assay quantifies the compound's ability to enhance neurotransmitter release.
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| Animal Protocol |
In vivo animal studies for DMP-543 are conducted in rodent models of cognitive impairment or epilepsy. The compound is administered orally, and its effects on cognitive performance, seizure threshold, or neurotransmitter levels in the brain are measured. Specific models are not detailed in the available sources.
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| ADME/Pharmacokinetics |
DMP-543 is an orally active compound. Its ability to enhance neurotransmitter release in vivo suggests good bioavailability and brain penetration. Its PK properties have been characterized in preclinical species.
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| Toxicity/Toxicokinetics |
Toxicological data for DMP-543 are not widely published. As a research compound, its safety profile has been evaluated in animal models. No significant toxicity has been reported in the available literature.
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| References |
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| Additional Infomation |
10,10-bis[(2-fluoro-4-pyridyl)methyl]-9-anthrone is a member of the anthracene class of compounds.
DMP-543 is also known as XR-543. It is a KV7 channel blocker and neurotransmitter release enhancer. It has been studied for its potential in treating cognitive disorders. It is not an approved drug. |
| Molecular Formula |
C26H18F2N2O
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|---|---|
| Molecular Weight |
412.4398
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| Exact Mass |
412.139
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| Elemental Analysis |
C, 75.72; H, 4.40; F, 9.21; N, 6.79; O, 3.88
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| CAS # |
160588-45-4
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| PubChem CID |
9887884
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| Appearance |
White to yellow solid powder
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| Density |
1.319g/cm3
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| Boiling Point |
593.1ºC at 760mmHg
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| Flash Point |
312.5ºC
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| Vapour Pressure |
0mmHg at 25°C
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| Index of Refraction |
1.643
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| LogP |
5.07
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
31
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| Complexity |
591
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC1C=C(CC2(CC3C=CN=C(F)C=3)C3C(=CC=CC=3)C(=O)C3=C2C=CC=C3)C=CN=1
|
| InChi Key |
MUJBUUDUXGDXLW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C26H18F2N2O/c27-23-13-17(9-11-29-23)15-26(16-18-10-12-30-24(28)14-18)21-7-3-1-5-19(21)25(31)20-6-2-4-8-22(20)26/h1-14H,15-16H2
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| Chemical Name |
10,10-bis[(2-fluoropyridin-4-yl)methyl]anthracen-9-one
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| Synonyms |
DMP543; XR-543; DMP-543
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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 (~242.47 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (6.06 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
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 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL 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: 2.5 mg/mL (6.06 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. 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 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4246 mL | 12.1230 mL | 24.2460 mL | |
| 5 mM | 0.4849 mL | 2.4246 mL | 4.8492 mL | |
| 10 mM | 0.2425 mL | 1.2123 mL | 2.4246 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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