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Description: Highly potent and selective PSAM4-GlyR and PSAM4-5-HT3 chimeric ion channel agonist; brain-penetrant
Chemical Name: 2-Propoxy-7,8,9,10-tetrahydro-6H-6,10-methanoazepino[4,5-g]quinoxaline L-tartrate
Purity: ≥98% (HPLC)
Biological Activity for uPSEM 817 tartrate
uPSEM 817 tartrate is a selective ultrapotent PSEM (uPSEM) agonist for α7L131G,Q139L,Y217F-GlyR (PSAM4-GlyR) and PSAM4-5-HT3 chimeric ion channels (EC50 values are 0.3 and 0.5 nM, respectively). Suppresses firing of layer 2/3 cortical neurons expressing PSAM4-GlyR in brain slices. Increases contralateral rotation in mice expressing PSAM4-GlyR unilaterally in the substantia nigra reticulata (LED 0.1 mg/kg).
Licensing Information
Sold under license from the Howard Hughes Medical Institute, Janelia Research Campus.
For scientific research use only. This product may not be used to research, develop, make, use, offer to sell, sell, or import any products for human therapeutic uses.
Technical Data for uPSEM 817 tartrate
| M. Wt | 419.43 |
| Formula | C16H19N3O.C4H6O6 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 2341833-14-3 |
| Smiles | CCCOC1=NC2=C(N=C1)C=C(C3=C2)C4CNCC3C4.O[C@@H](C(O)=O)[C@@H](O)C(O)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for uPSEM 817 tartrate
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 41.94 | 100 | |
| water | 8.39 | 20 |
Preparing Stock Solutions for uPSEM 817 tartrate
The following data is based on the product molecular weight 419.43. Batch specific molecular weights may vary from batch to batch due to the degree 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 | 2.38 mL | 11.92 mL | 23.84 mL |
| 5 mM | 0.48 mL | 2.38 mL | 4.77 mL |
| 10 mM | 0.24 mL | 1.19 mL | 2.38 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.48 mL |
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Product Datasheets for uPSEM 817 tartrate
References for uPSEM 817 tartrate
References are publications that support the biological activity of the product.
Magnus et al (2019) Ultrapotent chemogenetics for research and potential clinical applications. Science 364 PMID: 30872534
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Citations for uPSEM 817 tartrate
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Chemogenetics Research Bulletin
Produced by Tocris, the chemogenetics research bulletin provides an introduction to chemogenetic methods to manipulate neuronal activity. It outlines the development of RASSLs, DREADDs and PSAMs, and the use of chemogenetic compounds. DREADD ligands and PSEMs available from Tocris are highlighted.