Size
50.0mg; 100.0mg; 200.0mg; 500.0mg; 1.0g; 2.0g
Description
NS-11394 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.
Chemical Formula
C23H19N3O
Elemental Analysis
C, 78.16; H, 5.42; N, 11.89; O, 4.53
Synonym
NS-11394; NS 11394; NS11394.
IUPAC/Chemical Name
3'-(5-(2-hydroxypropan-2-yl)-1H-benzo[d]imidazol-1-yl)-[1,1'-biphenyl]-2-carbonitrile
InChi Key
HLKYSQGBIIIQJN-UHFFFAOYSA-N
InChi Code
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 Code
N#CC1=CC=CC=C1C2=CC=CC(N3C4=CC=C(C(C)(O)C)C=C4N=C3)=C2
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4℃ for short term (days to weeks), or -20℃ for long term (months).
HS Tariff Code
2934.99.9001