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NS11394

Overview
Catalog # bs-6628c-10mg-solid
Product Name NS11394
Specifications
Storage Buffer Powder
Storage Condition Store in dry, dark place at -20C for 1 year.
Target
Product Information Molecular Weight: 353.42

Formula: C23 H19 N3 O

CAS Number: 951650-22-9

InChi Key: HLKYSQGBIIIQJN-UHFFFAOYSA-N

InChi: InChI=1S/C23H19N3O/c1-23(2,27)18-10-11-22-21(13-18)25-15-26(22)19-8-5-7-16(12-19)20-9-4-3-6-17(20)14-24/h3-13,15,27H,1-2H3

Smiles: CC(C)(O)C1=CC2N=CN(C=2C=C1)C1C=C(C=CC=1)C1=CC=CC=C1C#N

Purity: 98.0

Solubility: Soluble in DMSO, not in water

Appearance: Solid Power.

Shelf Life: 1.0 years
Description NS11394 is a drug which acts as a subtype-selective positive allosteric modulator at GABAA receptors, with selectivity for the α3 and α5 subtypes. NS-11394 has been researched as an analgesic for use in chronic or neuropathic pain. NS-11394 possesses a functional selectivity profile at GABA(A) receptors of alpha(5) > alpha(3) > alpha(2) > alpha(1) based on oocyte electrophysiology with human GABA(A) receptors. Compared with other subtype-selective ligands, NS11394 is unique in having superior efficacy at GABA(A)-alpha(3) receptors while maintaining low efficacy at GABA(A)-alpha(1) receptors. NS11394 has an excellent pharmacokinetic profile, which correlates with pharmacodynamic endpoints (CNS receptor occupancy). NS11394 is potent and highly effective in rodent anxiety models. NS11394 has a significantly reduced side effect profile in rat (sedation, ataxia, and ethanol interaction) and mouse (sedation), even at full CNS receptor occupancy. NS11394 has a unique subtype-selective GABA(A) receptor profile and represents an excellent pharmacological tool to further understanding on the relative contributions of GABA(A) receptor subtypes in various therapeutic areas.