Biological Activity
Voltage- and use-dependent open-channel antagonist of AMPA receptors. Selective between subtypes; blocks GluR2 subunit-lacking receptors more potently than GluR2-containing receptors (KD for GluR2-containing AMPAR is 210 times higher at -80 mV). More potent than IEM 1460 (Cat. No. 1636) and IEM 1754 (Cat. No. 4199) due to a slower unblocking rate. Alleviates inflammatory pain in a rat model of peripheral inflammation.
Technical Data
| M. Wt | 422.24 |
| Formula | C17H28N2.2HBr |
| Storage | Desiccate at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 258282-23-4 |
| PubChem ID | 44561101 |
| InChI Key | ZCYUSVRXEKAQSL-UHFFFAOYSA-N |
| Smiles | NCCCCCNC1(C2=CC=CC=C2)CCCCC1.Br.Br |
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 | 21.11 | 50 | |
| water | 42.22 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 422.24. 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 | 2.37 mL | 11.84 mL | 23.68 mL |
| 5 mM | 0.47 mL | 2.37 mL | 4.74 mL |
| 10 mM | 0.24 mL | 1.18 mL | 2.37 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.47 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Tikhonov et al (2000) Voltage-dependent block of native AMPA receptor channels by dicationic compounds. Br.J.Pharmacol. 129 265 PMID: 10694232
Kopach et al (2016) Inhibition of spinal Ca2+-permeable AMPA receptors with dicationic compounds alleviates persistent inflammatory pain without adverse effects. Front.Cell Neurosci. 10 PMID: 26973464
Keywords: IEM 1925 dihydrobromide, supplier, IEM1925, 2HBr, AMPAR, antagonist, blocks, AMPA, receptor, voltage-dependent, channel, blocker, AMPA, Receptors, AMPA, Receptors, Tocris Bioscience
