Biological Activity
Positive allosteric modulator of muscarinic M1 receptors (EC50 = 198 nM). Displays no activity at M2-M5 at concentrations up to 30 μM. Potentiates NMDA receptor currents in hippocampal neurons; activity reverses cognitive decifits in a rodent model of hippocampal-dependent memory. CNS penetrant.
Technical Data
| M. Wt | 369.89 |
| Formula | C18H27N3O3.HCl |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1135242-13-5 |
| PubChem ID | 25010775 |
| InChI Key | XKJQVUIXSBOCPP-UHFFFAOYSA-N |
| Smiles | CC1=CC=CC=C1C(NCCNC2CCN(C(OCC)=O)CC2)=O.Cl |
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 | 1.85 | 5 | |
| water | 9.25 | 25 |
Preparing Stock Solutions
The following data is based on the product molecular weight 369.89. 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 | 2.7 mL | 13.52 mL | 27.04 mL |
| 5 mM | 0.54 mL | 2.7 mL | 5.41 mL |
| 10 mM | 0.27 mL | 1.35 mL | 2.7 mL |
| 50 mM | 0.05 mL | 0.27 mL | 0.54 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Bridges et al (2010) Chemical lead optimization of a pan Gq mAChR M1, M3, M5 positive allosteric modulator (PAM) Lead. Part II. Development of potent and highly selective M1 PAM. Bioorg.Med.Chem.Lett. 20 1972 PMID: 20156687
Lebois et al (2010) Discovery and characterization of novel subtype-selective allosteric agonists for the investigation of M1 receptor function in the central nervous system. ACS Chem.Neurosci. 1 104 PMID:
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