WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 522381
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.
MedKoo Cat#: 522381
Chemical Formula: C23H19N3O
Exact Mass: 353.15281
Molecular Weight: 353.42
Elemental Analysis: C, 78.16; H, 5.42; N, 11.89; O, 4.53
NS-11394, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.
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
The following data is based on the product molecular weight 353.42 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.15 mL||5.76 mL||11.51 mL|
|5 mM||0.23 mL||1.15 mL||2.3 mL|
|10 mM||0.12 mL||0.58 mL||1.15 mL|
|50 mM||0.02 mL||0.12 mL||0.23 mL|
1: Hofmann M, Kordás KS, Gravius A, Bölcskei K, Parsons CG, Dekundy A, Danysz W, Dézsi L, Wittko-Schneider IM, Sághy K, Gyertyán I, Horváth C. Assessment of the effects of NS11394 and L-838417, α2/3 subunit-selective GABA(A) [corrected] receptor-positive allosteric modulators, in tests for pain, anxiety, memory and motor function. Behav Pharmacol. 2012 Dec;23(8):790-801. doi: 10.1097/FBP.0b013e32835a7c7e. Erratum in: Behav Pharmacol. 2013 Apr;24(2):153. PubMed PMID: 23075708.
2: Hansen RR, Erichsen HK, Brown DT, Mirza NR, Munro G. Positive allosteric modulation of GABA-A receptors reduces capsaicin-induced primary and secondary hypersensitivity in rats. Neuropharmacology. 2012 Dec;63(8):1360-7. doi: 10.1016/j.neuropharm.2012.08.002. Epub 2012 Aug 17. PubMed PMID: 22985969.
3: Mirza NR, Larsen JS, Mathiasen C, Jacobsen TA, Munro G, Erichsen HK, Nielsen AN, Troelsen KB, Nielsen EØ, Ahring PK. NS11394 [3'-[5-(1-hydroxy-1-methyl-ethyl)-benzoimidazol-1-yl]-biphenyl-2-carbonitrile], a unique subtype-selective GABAA receptor positive allosteric modulator: in vitro actions, pharmacokinetic properties and in vivo anxiolytic efficacy. J Pharmacol Exp Ther. 2008 Dec;327(3):954-68. doi: 10.1124/jpet.108.138859. Epub 2008 Sep 12. PubMed PMID: 18791063.
4: Munro G, Lopez-Garcia JA, Rivera-Arconada I, Erichsen HK, Nielsen EØ, Larsen JS, Ahring PK, Mirza NR. Comparison of the novel subtype-selective GABAA receptor-positive allosteric modulator NS11394 [3'-[5-(1-hydroxy-1-methyl-ethyl)-benzoimidazol-1-yl]-biphenyl-2-carbonitrile] with diazepam, zolpidem, bretazenil, and gaboxadol in rat models of inflammatory and neuropathic pain. J Pharmacol Exp Ther. 2008 Dec;327(3):969-81. doi: 10.1124/jpet.108.144568. Epub 2008 Sep 12. PubMed PMID: 18791060.