| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
AMPA receptor (antagonist), NMDA receptor (antagonist), and kainate receptor (GluK1, GluK2). NS-102 is a glutamate receptor antagonist that inhibits AMPA, NMDA, and kainate receptor activity.
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| ln Vitro |
When NS-102 (10 μM) and GYKI 52466 (30 μM) are combined, compound action potential (CAP) is not completely lost during oxygen and glucose deprivation (OGD) and the CAP area recovers more quickly [1].
NS-102 is a glutamate receptor antagonist that inhibits AMPA binding with an IC50 of 7.2 μM. It blocks GluK1-containing KARs on DRG neurons with a Kb of 6 μM and has weaker effects at native AMPARs in the cortex (114 μM). It inhibits erythrocyanine (GluK2), reducing GluR6 receptor-mediated currents. In vitro, NS-102 (10 μM) in combination with GYKI 52466 (30 μM) prevented the complete loss of the compound action potential (CAP) during OGD and increased CAP area recovery. |
| ln Vivo |
The hippocampal CA3 region treated with NS-102 (20, 40, or 80 μMol) dramatically lessens sevoflurane-induced ADHD [1].
In vivo, NS-102 produced significant reductions in overall toxicity, onset of motor seizures, and hippocampal CA3 cell damage induced by domoic acid at doses that did not antagonize kainic acid-induced toxicity. This indicates that domoic acid toxicity in vivo is mediated largely by a non-NMDA receptor, likely the kainate receptor. |
| Enzyme Assay |
In vitro receptor binding assays for NS-102 are performed to evaluate its affinity for AMPA, NMDA, and kainate receptors. Radioligand binding studies using membrane preparations from cells or tissues expressing the target receptors are conducted. The compound's ability to displace specific radiolabeled ligands, such as [3H]AMPA or [3H]kainate, is measured to calculate its IC50 values. Functional assays, such as electrophysiological recordings, are used to confirm its antagonist activity at these receptors.
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| Cell Assay |
In vitro cell-based assays are conducted using cells expressing AMPA, NMDA, or kainate receptors. The cells are treated with receptor agonists in the presence or absence of NS-102, and receptor activity is measured by assessing downstream signaling events such as calcium mobilization or electrophysiological responses. The compound's ability to inhibit agonist-induced responses is quantified. In OGD models, the protective effect of NS-102 on compound action potentials is assessed.
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| Animal Protocol |
In vivo animal studies are conducted to evaluate the effects of NS-102 on domoic acid-induced toxicity. The compound is administered via various routes, and its effects on toxicity, seizure onset, and hippocampal cell damage are assessed in rodent models. Dosing regimens are determined based on preliminary dose-response studies.
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| ADME/Pharmacokinetics |
No detailed pharmacokinetic data are publicly available for NS-102. As a research compound, its ADME properties would be characterized in standard preclinical studies to guide in vivo experiments. The compound's ability to cross the blood-brain barrier is a key parameter for its use in CNS research.
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| Toxicity/Toxicokinetics |
No specific toxicity data are publicly available for NS-102. As a glutamate receptor antagonist, its toxicity profile would be expected to be related to its mechanism of action. Excessive inhibition of glutamatergic neurotransmission can impair synaptic plasticity and cognitive function.
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| References |
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| Additional Infomation |
NS-102 is a nitronaphthalene.
NS-102 is a glutamate receptor antagonist that inhibits AMPA, NMDA, and kainate receptor activity. It has been shown to block GluK1-containing KARs (Kb = 6 μM) and inhibit AMPA binding (IC50 = 7.2 μM). In vivo, it reduces domoic acid-induced toxicity and seizures. NS-102 is a research tool for studying glutamate receptor function and is not approved for human therapeutic use. |
| Molecular Formula |
C12H11N3O4
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|---|---|
| Molecular Weight |
261.23
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| Exact Mass |
261.075
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| CAS # |
136623-01-3
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| PubChem CID |
4461601
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| Appearance |
Off-white to yellow solid powder
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| Density |
1.74g/cm3
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| Boiling Point |
405.8ºC at 760mmHg
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| Flash Point |
199.2ºC
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| Vapour Pressure |
2.81E-08mmHg at 25°C
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| Index of Refraction |
1.794
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| LogP |
2.132
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
19
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| Complexity |
386
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1CCC2=C3C(=CC(=C2C1)[N+](=O)[O-])C(=C(N3)O)N=O
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| InChi Key |
SADZJARZJNQZHT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C12H11N3O4/c16-12-11(14-17)8-5-9(15(18)19)6-3-1-2-4-7(6)10(8)13-12/h5,13,16H,1-4H2
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| Chemical Name |
5-nitro-3-nitroso-6,7,8,9-tetrahydro-1H-benzo[g]indol-2-ol
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 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) |
DMSO: 4 mg/mL (15.31 mM)
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.8280 mL | 19.1402 mL | 38.2804 mL | |
| 5 mM | 0.7656 mL | 3.8280 mL | 7.6561 mL | |
| 10 mM | 0.3828 mL | 1.9140 mL | 3.8280 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.
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