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uPSEM 792 hydrochloride

Catalog #: 6865 Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
6865/5
6865/25
uPSEM 792 hydrochloride | CAS No. 2341841-08-3 | PSEMs
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Description: Highly potent PSAM4-GlyR and PSAM4-5-HT3 chimeric ion channel agonist; brain-penetrant

Chemical Name: 1-Methyl-7,8,9,10-tetrahydro-1H-6,10-methanoazepino[4,5-g]quinoxalin-2(6H)-one hydrochloride

Purity: ≥98%

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Biological Activity

uPSEM 792 hydrochloride is a ultrapotent PSEM (uPSEM) agonist for PSAM4-GlyR and PSAM4-5HT3 (Ki = 0.7 nM for PSAM4-GlyR and <10 nM for PSAM4-5HT3). Exhibits >10,000-fold agonist selectivity for PSAM4-GlyR over α7-GlyR, α7-5HT3, and 5HT3-R, and 230-fold selectivity over α4β2 nAChR. Also weak partial agonist (~10 %) at α4β2 nAChR. Retains the potency of varenicline (Cat.No. 3754) for PSAM4-GlyR with enhanced chemogenetic selectivity. Does not act as a substrate for P-glycoprotein pumps. Silences neurons in vivo. Brain-penetrant.

Technical Data

M.Wt:
277.75
Formula:
C14H15N3O.HCl
Solubility:
Soluble to 100 mM in water
Purity:
≥98%
Storage:
Store at -20°C
CAS No:
2341841-08-3

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.

Additional Information

Licensing Caveats:
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.

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