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Purity: ≥98%
NS11394 is a potent, selective and novel positive allosteric modulator of GABA(A) receptor. NS11394 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), 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.
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In the formalin test, NS11394 (1-120 mg/kg) selectively reduces injury-induced nociceptive behaviors[2]. In CFA rats, NS11394 (1–10 mg/kg) significantly reduces the hindpaw weight bearing deficit [F(4,61) = 7.569, p < 0.001][2].
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| Animal Protocol |
Animal/Disease Models: Adult male SD (Sprague-Dawley) rats[2].
Doses: 1-120 mg/kg. Route of Administration: Orally. Experimental Results: Dramatically attenuated motor function compared with corresponding vehicle responses. Dramatically decreased flinching behavior during interphase [F(3,30) = 4.139, p < 0.05] and the second phase [F(3,30) = 11.033, p < 0.001] of the formalin test compared with vehicle treatment indicative of a selective effect on injury-induced nociceptive transmission. |
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| References |
[1]. N. R. Mirza, 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 Effica
[2]. G. Munro, J. A., 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 [3]. Martine Hofmann, et al. Assessment of the effects of NS11394 and L-838417, a2/3 subunit-selective GABAA receptor-positive allosteric modulators, in tests for pain, anxiety, memory and motor function. Behavioural Pharmacology 2012, 23:790–801. |
| Molecular Formula |
C23H19N3O
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| Molecular Weight |
353.42
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| CAS # |
951650-22-9
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| SMILES |
N#CC1=CC=CC=C1C2=CC=CC(N3C4=CC=C(C(C)(O)C)C=C4N=C3)=C2
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.07 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.07 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.07 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8295 mL | 14.1475 mL | 28.2949 mL | |
| 5 mM | 0.5659 mL | 2.8295 mL | 5.6590 mL | |
| 10 mM | 0.2829 mL | 1.4147 mL | 2.8295 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
 In vitro efficacy of NS11394 in two-electrode voltage-clamp experiments at human recombinant GABAAreceptors expressed inX. laevisoocytes.J Pharmacol Exp Ther.2008 Dec;327(3):954-68. |
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 Top, effect of NS11394 (0.3–10 mg/kg p.o.,n= 7) on rat CER performance. A and B, mean light/dark and suppression ratio data, respectively. Bottom, effect of alprazolam (0.3–3 mg/kg i.p.,n= 6) on rat CER performance. C and D, mean light/dark and suppression ratio data, respectively.J Pharmacol Exp Ther.2008 Dec;327(3):954-68. |
 Top, effect of NS11394 (0.3–10 mg/kg p.o.,n= 10) (A) and chlordiazepoxide (5–20 mg/kg i.p.,n= 8–10) (B) in the mouse four-plate test. Bottom, effect of NS11394 (0.1–1 mg/kg p.o.,n= 8) and paroxetine (PRX, 10 mg/kg i.p.,n= 7) (C) and diazepam (0.1–3 mg/kg i.p.,n= 8) (d) in the mouse marble burying test.J Pharmacol Exp Ther.2008 Dec;327(3):954-68. |
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