Biological Activity
Positive allosteric modulator of α7 neuronal nicotinic acetylcholine receptors (nAChR). Evokes positive modulation of acetylcholine (ACh)-induced EC5 currents (EC50 = 0.7 μM). Exhibits cognitive-enhancing properties in rodent models; displays no cytotoxic effects in PC12 cells or rat primary cortical neurons.
Compound Libraries
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Technical Data
| M. Wt | 388.25 |
| Formula | C19H15Cl2N3O2 |
| Storage | Store at -20°C |
| CAS Number | 917837-54-8 |
| PubChem ID | 67042344 |
| InChI Key | VMAKIACTLSBBIY-UHFFFAOYSA-N |
| Smiles | CC1=NOC(=C1)C(=CNC1=CC=C(Cl)C=C1)C(=O)NC1=CC=C(Cl)C=C1 |
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 | 38.83 | 100 | |
| ethanol | 3.88 | 10 |
Preparing Stock Solutions
The following data is based on the product molecular weight 388.25. 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 | 2.58 mL | 12.88 mL | 25.76 mL |
| 5 mM | 0.52 mL | 2.58 mL | 5.15 mL |
| 10 mM | 0.26 mL | 1.29 mL | 2.58 mL |
| 50 mM | 0.05 mL | 0.26 mL | 0.52 mL |
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References
References are publications that support the products' biological activity.
Gronlien et al (2007) Distinct profiles of α7 nAChR positive allosteric modulation revealed by structurally diverse chemotypes. Mol.Pharmacol. 72 715 PMID: 17565004
Hu et al (2009) Positive allosteric modulation of α7 neuronal nicotinic acetylcholine receptors: lack of cytotoxicity in PC12 cells and rat primary cortical neurons. Br.J.Pharmacol. 158 1857 PMID: 20050184
Ng et al (2007) Nootropic α7 nicotinic receptor allosteric modulator derived from GABAA receptor modulators. Proc.Natl.Acad.Sci. 104 8059 PMID:
Keywords: CCMI, supplier, Positive, allosteric, modulators, α7, alpha7, a7, nAChR, Nicotinic, Receptors, Acetylcholine, XY4083, XY, 4083, Nicotinic, (a7), Receptors, Nicotinic, (a7), Receptors, Tocris Bioscience
