| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| 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].
|
|---|---|
| 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].
|
| 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 |
|
| Additional Infomation |
The structure given in the first document
|
| Molecular Formula |
C13H14O3
|
|---|---|
| Molecular Weight |
218.248464107513
|
| Exact Mass |
218.094
|
| CAS # |
520505-01-5
|
| Related CAS # |
NCS-382 sodium;131733-92-1
|
| PubChem CID |
5875451
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.3±0.1 g/cm3
|
| Boiling Point |
460.8±30.0 °C at 760 mmHg
|
| Flash Point |
246.6±21.1 °C
|
| Vapour Pressure |
0.0±1.2 mmHg at 25°C
|
| Index of Refraction |
1.682
|
| LogP |
2.17
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
1
|
| Heavy Atom Count |
16
|
| Complexity |
296
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
OC(/C=C1/CCCC2=CC=CC=C2[C@H]/1O)=O
|
| InChi Key |
UADPGHINQMWEAG-CSKARUKUSA-N
|
| InChi Code |
InChI=1S/C13H14O3/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)/b10-8+
|
| Chemical Name |
(2E)-2-(5-hydroxy-5,7,8,9-tetrahydrobenzo[7]annulen-6-ylidene)acetic acid
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| 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
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: NCS-382 dissolved in 0.1% sodium bicarbonate[1] (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.
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