uPSEM 817 tartrate

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Cat.No. 6866 - uPSEM 817 tartrate | C16H19N3O.C4H6O6
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)
Datasheet
Citations
Reviews
Literature

Biological Activity

Selective ultrapotent PSEM (uPSEM) agonist for α7L131G,Q139L,Y217F-GlyR (PSAM4-GlyR) and PSAM4-5-HT3 chimeric ion channel agonist (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

M. Wt 419.43
Formula C16H19N3O.C4H6O6
Storage Store at -20°C
Purity ≥98% (HPLC)
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

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 41.94 100
water 8.39 20

Preparing Stock Solutions

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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References

References are publications that support the biological activity of the product.

Magnus et al (2019) Ultrapotent chemogenetics for research and potential clinical applications. Science PMID: 30872534


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Literature in this Area

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Chemogenetics

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.