Product overview

Name uPSEM817 tartrate
Description Selective, ultrapotent PSEM agonist for PSAM4-GlyR and PSAM4-5HT3. Brain penetrant.
Purity >99%
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Biological Data

Biological description

Overview

Selective, ultrapotent PSEM agonist for PSAM4-GlyR and PSAM4-5HT3 (Ki values are 0.15 nM and and EC50 = 0.3 nM at PSAM4-GlyR) which can be used for targeted control of brain activity in rodent and primate models.

It has excellent selectivity with 5000- to 10,000-fold selectivity for PSAM4-GlyR over α-7-GlyR, α7-5HT3R and 5-HT3R. It also does not show evident α4β2 nAChR agonism up to 30 µM.

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
Storage buffer Soluble in DMSO (100 mM), and in water (50 mM, gentle warming)
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 2-Propoxy-7,8,9,10-tetrahydro-6H-6,10-methanoazepino[4,5-g]quinoxaline L-tartrate
Molecular Weight 419.43
Chemical structure uPSEM 817 tartrate Chemical Structure
Molecular Formula C16H19N3O.C4H6O6
PubChem identifier 138991793
SMILES CCCOC1=NC2=C(N=C1)C=C(C3=C2)C4CNCC3C4.O[C@@H](C(O)=O)[C@@H](O)C(O)=O
Source Synthetic
InChi InChI=1S/C16H19N3O.C4H6O6/c1-2-3-20-16-9-18-14-5-12-10-4-11(8-17-7-10)13(12)6-15(14)19-16;5-1(3(7)8)2(6)4(9)10/h5-6,9-11,17H,2-4,7-8H2,1H3;1-2,5-6H,(H,7,8)(H,9,10)/t;1-,2-/m.1/s1
InChiKey ATMVSWRWVDLFOP-LREBCSMRSA-N
Appearance Off-white 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 uPSEM817 tartrate

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 uPSEM817 tartrate 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 : Preprint

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