Biological Activity
Acetylcholine release stimulator. Potently enhances K+-stimulated [3H]-ACh release from rat hippocampal slices (EC50 = 700 nM), and increases release of dopamine and glutamate (EC50 values are 0.25 and 0.22 μM, respectively). Orally active in vivo; increases ACh levels in rats (with a minimum effective dose of 1 mg/kg) and exerts a long duration of action. More potent than linopirdine (Cat. No. 1999) both in vitro and in vivo. Also K+ channel blocker.
Compound Libraries
DMP 543 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 412.44 |
| Formula | C26H18F2N2O |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 160588-45-4 |
| PubChem ID | 9887884 |
| InChI Key | MUJBUUDUXGDXLW-UHFFFAOYSA-N |
| Smiles | FC1=CC(CC2(CC3=CC(F)=NC=C3)C3=CC=CC=C3C(=O)C3=C2C=CC=C3)=CC=N1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 41.24 | 100 | |
| ethanol | 20.62 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 412.44. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.42 mL | 12.12 mL | 24.25 mL |
| 5 mM | 0.48 mL | 2.42 mL | 4.85 mL |
| 10 mM | 0.24 mL | 1.21 mL | 2.42 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.48 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Zaczek et al (1998) Two new potent neurotransmitter release enhancers, 10,10-Bis(4-pyridinylmethyl)-9(10H)-anthracenone and 10,10-Bis(2-fluoro-4-pyridinylmethyl)-9(10H)-anthracenone: comparison to linopirdine. J.Pharmacol.Exp.Ther. 285 724 PMID: 9580619
Earl et al (1998) 2-Fluoro-4-pyridinylmethyl analogues of linopirdine as orally active acetylcholine release-enhancing agents with good efficacy and duration of action. J.Med.Chem. 41 4615 PMID: 9804701
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