NS-11394

Modify Date: 2024-01-03 00:32:17

NS-11394 Structure
NS-11394 structure
Common Name NS-11394
CAS Number 951650-22-9 Molecular Weight 353.417
Density 1.2±0.1 g/cm3 Boiling Point 623.7±65.0 °C at 760 mmHg
Molecular Formula C23H19N3O Melting Point N/A
MSDS N/A Flash Point 331.0±34.3 °C

 Use of NS-11394


NS11394 is a potent and subtype-selective GABA(A) receptor-positive modulator; possesses a functional efficacy selectivity profile of alpha(5) > alpha(3) > alpha(2) > alpha(1) at GABA(A) alpha subunit-containing receptors.IC50 value:Target: GABA A receptor modulatorin vitro: 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), yielding a high level of confidence in deriving in vivo conclusions anchored to an in vitro selectivity profile and allowing for translation to higher species [2]. in vivo: Oral administration of NS11394 (1-30 mg/kg) to rats attenuated spontaneous nociceptive behaviors in response to hindpaw injection of formalin and capsaicin, effects that were blocked by the benzodiazepine site antagonist flumazenil [1]. NS11394 impairs memory in both rats and mice, which is possibly attributable to its efficacy at GABA(A)-alpha(5) receptors, albeit activity at this receptor might be relevant to its antinociceptive effects [2].

 Names

Name 2-[3-[5-(2-hydroxypropan-2-yl)benzimidazol-1-yl]phenyl]benzonitrile
Synonym More Synonyms

 NS-11394 Biological Activity

Description NS11394 is a potent and subtype-selective GABA(A) receptor-positive modulator; possesses a functional efficacy selectivity profile of alpha(5) > alpha(3) > alpha(2) > alpha(1) at GABA(A) alpha subunit-containing receptors.IC50 value:Target: GABA A receptor modulatorin vitro: 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), yielding a high level of confidence in deriving in vivo conclusions anchored to an in vitro selectivity profile and allowing for translation to higher species [2]. in vivo: Oral administration of NS11394 (1-30 mg/kg) to rats attenuated spontaneous nociceptive behaviors in response to hindpaw injection of formalin and capsaicin, effects that were blocked by the benzodiazepine site antagonist flumazenil [1]. NS11394 impairs memory in both rats and mice, which is possibly attributable to its efficacy at GABA(A)-alpha(5) receptors, albeit activity at this receptor might be relevant to its antinociceptive effects [2].
Related Catalog
References

[1]. Munro G, et al. 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

[2]. Mirza NR, et al. 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.

 Chemical & Physical Properties

Density 1.2±0.1 g/cm3
Boiling Point 623.7±65.0 °C at 760 mmHg
Molecular Formula C23H19N3O
Molecular Weight 353.417
Flash Point 331.0±34.3 °C
Exact Mass 353.152802
PSA 61.84000
LogP 4.16
Appearance of Characters white solid
Vapour Pressure 0.0±1.9 mmHg at 25°C
Index of Refraction 1.637
Storage condition -20℃

 Synonyms

[1,1'-Biphenyl]-2-carbonitrile, 3'-[5-(1-hydroxy-1-methylethyl)-1H-benzimidazol-1-yl]-
NS-11394
3'-[5-(1-hydroxy-1-methyl-ethyl)-benzoimidazol-1-yl]-biphenyl-2-carbonitrile
3'-[5-(2-Hydroxy-2-propanyl)-1H-benzimidazol-1-yl]-2-biphenylcarbonitrile
NS11394
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