SJM-3 is a positive allosteric modulator of different isoforms of the GABAA receptor. SJM-3 binds at the high-affinity benzodiazepine binding site at the α+/γ- subunit interface.

Product information

CAS Number: 1234977-97-9

Molecular Weight: 354.40

Formula: C18H15FN4OS

Chemical Name: 6-fluoro-2-methyl-1-[2-(pyrazin-2-yl)-1,3-thiazole-4-carbonyl]-1,2,3,4-tetrahydroquinoline

Smiles: CC1CCC2C=C(F)C=CC=2N1C(=O)C1=CSC(=N1)C1=CN=CC=N1

InChiKey: MCMRMBOJJFVNHG-UHFFFAOYSA-N

InChi: InChI=1S/C18H15FN4OS/c1-11-2-3-12-8-13(19)4-5-16(12)23(11)18(24)15-10-25-17(22-15)14-9-20-6-7-21-14/h4-11H,2-3H2,1H3

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

SJM-3 binds at the high-affinity benzodiazepine binding site at theα+/γ- subunit interface but effects its action through another site presumably located within the transmembrane domain. The binding affinity of SJM-3 at wild type receptors is determined by displacement of [3H]-Flunitrazepam and [3H]-Ro15-1788 and indicates a Ki of SJM-3 amounting to 218±70 nM and 242±38 nM, respectively.

References:

1. Middendorp SJ, Maldifassi MC, Baur R, Sigel E. Positive modulation of synaptic and extrasynaptic GABAA receptors by an antagonist of the high affinity benzodiazepine binding site. Neuropharmacology. 2015 Aug;95:459-67.

Products are for research use only. Not for human use.