Biological Activity
AMPA receptor antagonist. Non-selective homomeric GluR3 and GluR1 receptor antagonist (IC50 values are 263 and 296 nM respectively). Inhibits homomeric GluR3 and GluR1 with a 100-fold greater potency than heteromeric GluR1/2 and GluR2/3 receptors.
Technical Data
| M. Wt | 507.54 |
| Formula | C24H42N4O3.2HCl |
| Storage | Desiccate at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 1227301-51-0 |
| PubChem ID | 46213501 |
| InChI Key | HWTJQQMIKVJWLH-IKXQUJFKSA-N |
| Smiles | OC1=CC=C(C[C@H](NC(CCC)=O)C(NCCCCCCCNCCCCN)=O)C=C1.Cl.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 | 50.75 | 100 | |
| water | 50.75 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 507.54. 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 | 1.97 mL | 9.85 mL | 19.7 mL |
| 5 mM | 0.39 mL | 1.97 mL | 3.94 mL |
| 10 mM | 0.2 mL | 0.99 mL | 1.97 mL |
| 50 mM | 0.04 mL | 0.2 mL | 0.39 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Nilsen and England (2007) A subtype-selective, use-dependent inhibitor of native AMPA receptors. J.Am.Chem.Soc. 129 4902 PMID: 17391037
Poulsen et al (2013) Evaluation of PhTX-74 as subtype-selective inhibitor of GluA2-containing AMPA receptors. Mol.Pharmacol. 85 261 PMID: 24220009
Keywords: Philanthotoxin 74, supplier, GluR1/2, selective, AMPA, antagonists, Glutamate, Receptors, iGluR, Ionotropic, Philanthotoxin74, PhTx74, homomeric, GluR3, GluR1, GluR2/3, PhTx-74, AMPA, Receptors, AMPA, Receptors, Tocris Bioscience
