Product overview

Name uPSEM792 hydrochloride
Description Ultrapotent PSEM agonist for PSAM4-GlyR and PSAM4-5HT3. Brain penetrant.
Purity >99%
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Biological Data

Biological description

Overview

Ultrapotent PSEM agonist for PSAM4-GlyR and PSAM4-5HT3 (Ki values are 0.7 nM and <10 nM for PSAM4-GlyR and PSAM4-5HT3 respectively) which can be used for targeted control of brain activity in rodent and primate models.

It shows >10,000-fold agonist selectivity for PSAM4-GlyR over α-7-GlyR, α7-5HT3R and 5-HT3R.

uPSEM792 is a very weak agonist at α4β2 nAChR and shows 230-fold selectivity for PSAM4-GlyR over α4β2 nAChR.

It retains the potency of varenicline for PSAM4-GlyR with enhanced chemogenetic selectivity.

It does not act as a P-glycoprotein pump (PgP) substrate.

Uses and applications

It strongly suppresses layer 2/3 cortical neurons expressing PSAM4-GlyR in brain slices at low concentrations (ranging from 1-15 nM).

Solubility & Handling

Storage instructions -20°C
Solubility overview Soluble in water (100 mM)
Important This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use

Calculators

Molarity

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Dilution

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Chemical Data

Chemical name 1-Methyl-7,8,9,10-tetrahydro-1H-6,10-methanoazepino[4,5-g]quinoxalin-2(6H)-one hydrochloride
Molecular Weight 277.75
Chemical structure uPSEM792 hydrochloride Chemical Structure
Molecular Formula C14H15N3O · HCl
PubChem identifier 138991792
SMILES CN1C2=C(C=C3C4CC(C3=C2)CNC4)N=CC1=O.Cl
InChi InChI=1S/C14H15N3O.ClH/c1-17-13-4-11-9-2-8(5-15-6-9)10(11)3-12(13)16-7-14(17)18;/h3-4,7-9,15H,2,5-6H2,1H3;1H
InChiKey CDHPEJUYEXNGCV-UHFFFAOYSA-N
Appearance Yellow solid
Licensing details 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.

References for uPSEM792 hydrochloride

References are publications that support the biological activity of the product
  • Ultrapotent chemogenetics for research and potential clinical applications.

    Magnus CJ et al (2019) Science 364(6436) : 5282
Publications
These publications cite the use of uPSEM792 hydrochloride purchased from Hello Bio:
  • Characterization of ultrapotent chemogenetic ligands for research applications in non-human primates

    Raper et al (2022) https://www.biorxiv.org/content/10.1101/2022.01.06.475241v1.abstract : Preprint

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