| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
GHB receptor (γ-hydroxybutyrate receptor) and GABA receptor. NCS-382 sodium is a potent antagonist of the GHB receptor and has also been described as a GABA receptor antagonist.
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|---|---|
| ln Vitro |
NCS-382 sodium is a potent GHB receptor antagonist with IC50 values of 134.1 nM in rat striatal membranes and 201.3 nM in rat hippocampal membranes in radioligand binding assays. It is selective for the GHB receptor over GABA binding sites in rat brain synaptic membranes at concentrations of 1 and 10 µM. NCS-382 sodium has anti-sedative and anti-hypnotic properties.
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| ln Vivo |
In vivo, NCS-382 sodium has anti-sedative and anti-hypnotic activities. As a GHB receptor antagonist, it blocks the effects of GHB and related compounds.
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| Enzyme Assay |
In vitro receptor binding assays for NCS-382 sodium are performed to evaluate its affinity for the GHB receptor. Radioligand binding studies using membrane preparations from rat striatal and hippocampal membranes are conducted. The compound's ability to displace a specific radiolabeled GHB ligand is measured to calculate its IC50 values. Selectivity over GABA binding sites is confirmed by testing its activity at GABA receptors.
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| Cell Assay |
In vitro cell-based assays are conducted using cells expressing the GHB receptor. The cells are treated with NCS-382 sodium, and receptor antagonism is measured by assessing its ability to block GHB-induced downstream signaling events.
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| Animal Protocol |
In vivo animal studies with NCS-382 sodium are conducted in rodent models to evaluate its anti-sedative and anti-hypnotic effects. The compound is typically administered via intraperitoneal or intravenous injection. Its ability to reverse GHB-induced sedation or hypnosis is assessed.
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| ADME/Pharmacokinetics |
No detailed pharmacokinetic data are publicly available for NCS-382 sodium. As a small molecule antagonist, its ADME properties would be characterized in standard preclinical studies.
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| Toxicity/Toxicokinetics |
No specific toxicity data are publicly available for NCS-382 sodium. As a GHB receptor antagonist, its toxicity profile would be expected to be related to its mechanism of action.
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| References | |
| Additional Infomation |
NCS-382 sodium is a potent GHB receptor antagonist with IC50 values of 134.1 nM and 201.3 nM in rat striatal and hippocampal membranes, respectively. It is selective for the GHB receptor over GABA binding sites and has anti-sedative and anti-hypnotic properties. NCS-382 sodium is a valuable research tool for studying the GHB receptor and GHB pharmacology. The compound is not approved for human therapeutic use and is strictly for research purposes.
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| Molecular Formula |
C13H13NAO3
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|---|---|
| Molecular Weight |
240.23
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| Exact Mass |
240.076
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| CAS # |
131733-92-1
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| Related CAS # |
NCS-382;520505-01-5
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| PubChem CID |
3613485
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| Appearance |
White to off-white solid powder
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| Density |
1.34g/cm3
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| Boiling Point |
460.8ºC at 760mmHg
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| Melting Point |
141-143ºC
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| Flash Point |
246.6ºC
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| Vapour Pressure |
2.74E-09mmHg at 25°C
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| LogP |
0.732
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
17
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| Complexity |
301
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1CC2=CC=CC=C2C(C(=CC(=O)[O-])C1)O.[Na+]
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| InChi Key |
BTWDZCORIHHOPO-UHFFFAOYSA-M
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| InChi Code |
InChI=1S/C13H14O3.Na/c14-12(15)8-10-6-3-5-9-4-1-2-7-11(9)13(10)16;/h1-2,4,7-8,13,16H,3,5-6H2,(H,14,15);/q;+1/p-1
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| Chemical Name |
sodium;2-(5-hydroxy-5,7,8,9-tetrahydrobenzo[7]annulen-6-ylidene)acetate
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 4.1627 mL | 20.8134 mL | 41.6268 mL | |
| 5 mM | 0.8325 mL | 4.1627 mL | 8.3254 mL | |
| 10 mM | 0.4163 mL | 2.0813 mL | 4.1627 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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