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100mg | ||
250mg | ||
500mg | ||
Other Sizes |
ln Vitro |
HepG2 cells do not exhibit the capacity of NCS-382 (0.5 nM, 24 h) to inhibit microsomal CYPs (CYP1A2, 2B6, 2C8, 2C9, 2C19, 2D6, and 3A4) [2]. For HepG2 cells, NCS-382 (0.01-1000 μM, 24 h) exhibits minimal cytotoxicity [2]. The GHBR antagonist NCS-382 has IC50 values in isolated rat striatum and hippocampus membranes of 134.1 and 201.3 nM, respectively [4].
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ln Vivo |
In mice models, at a dose of 100 mg/kg, the maximum serum concentration was four times that in brain tissue, ten times that in kidney tissue, and the greatest concentration in liver tissue was NCS-382 (100, 300, 500 mg/kg; i.p.). Serum concentrations are more than 700% greater[1]. In mice models, after intraperitoneal treatment at a dose of 100 mg/kg, it may reside more favorably in the liver but stay longer in the brain and kidneys. An increase in the brain-to-serum ratio in a mouse model indicated that the 500 mg/kg dose improved brain permeability. When given at doses of 1.66 mmol/kg and 2.08 mmol/kg, NCS-382 (0.83-2.08 mmol/kg/kg; i.p.) decreases GHB-induced stress in the forced swim test in mouse models. The longer amount of time spent at rest suggests anti-sedative action[3]. In a rat model of miniature epilepsy and in Swiss RB mice prone to audiogenic epilepsy, NCS-382 (2.3 mmol/kg/kg; i.p.) attenuates spike and wave discharges[4].
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Cell Assay |
Cell Cytotoxicity Assay[2]
Cell Types: HepG2 cells Tested Concentrations: 0.01-1000 μM Incubation Duration: 24 h Experimental Results: diminished HepG2 cell viability at a concentration of 1 mM, and this same concentration did not induce apoptosis or cytotoxicity in HepG2 cells. |
Animal Protocol |
Animal/Disease Models: GBL induced mouse model[1]
Doses: 300 mg/kg(Combined with diclofenac (25 mg/kg)) Route of Administration: intraperitoneal (ip) injection (ip), Thirty minutes later, mice were given an ip injection of GBL (100 mg /kg diluted in PBS) Experimental Results: In the presence of diclofenac, it was highly protective against GBL mediated responses. Animal/Disease Models: GBL induced mouse model[3] Doses: 0.83, 1.25, 1.66, 2.08mmol/kg Route of Administration: intraperitoneal (ip) injection ( ip), 30 min before the test Experimental Results: At a dosage of 2.08 mmol/kg, completely blocked the effect of GHB when administered at 3.18 mmol/kg |
References |
[1]. Ainslie GR, et al. A pharmacokinetic evaluation and metabolite identification of the GHB receptor antagonist NCS-382 in mouse informs novel therapeutic strategies for the treatment of GHB intoxication. Pharmacol Res Perspect. 2016 Oct 18;4(6):e00265.
[2]. Vogel KR, et al. In vitro toxicological evaluation of NCS-382, a high-affinity antagonist of γ-hydroxybutyrate (GHB) binding. Toxicol In Vitro. 2017 Apr;40:196-202 [3]. Schmidt C, et al. Anti-sedative and anti-cataleptic properties of NCS-382, a gamma-hydroxybutyrate receptor antagonist. Eur J Pharmacol. 1991 Oct 22;203(3):393-7. [4]. Maitre M, Hechler V, Vayer P, Gobaille S, Cash CD, Schmitt M, Bourguignon JJ. A specific gamma-hydroxybutyrate receptor ligand possesses both antagonistic and anticonvulsant properties. J Pharmacol Exp Ther. 1990 Nov;255(2):657-63. |
Molecular Formula |
C13H14O3
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Molecular Weight |
218.25
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CAS # |
520505-01-5
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Related CAS # |
NCS-382 sodium;131733-92-1
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
OC(/C=C1/CCCC2=CC=CC=C2[C@H]/1O)=O
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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 | 4.5819 mL | 22.9095 mL | 45.8190 mL | |
5 mM | 0.9164 mL | 4.5819 mL | 9.1638 mL | |
10 mM | 0.4582 mL | 2.2910 mL | 4.5819 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.