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Gavestinel (GV 150526) is a non-competitive NMDA receptor antagonist that is potent, selective and orally active.Gavestinel binds to the glycine site of the NMDA receptor with a binding affinity (pKi value) of 8.5.Gavestinel is used in acute ischaemic stroke studies.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $38 | In Stock | In Stock | |
| 5 mg | $89 | In Stock | In Stock | |
| 10 mg | $147 | In Stock | In Stock | |
| 25 mg | $248 | In Stock | In Stock | |
| 50 mg | $369 | In Stock | In Stock | |
| 100 mg | $543 | - | In Stock |
| Description | Gavestinel (GV 150526) is a non-competitive NMDA receptor antagonist that is potent, selective and orally active.Gavestinel binds to the glycine site of the NMDA receptor with a binding affinity (pKi value) of 8.5.Gavestinel is used in acute ischaemic stroke studies. |
| Targets&IC50 | NMDAR:8.5(pKi) |
| In vivo | Gavestinel (800 mg) was administered as a loading dose and followed by either 100 mg, 200 mg, or 400 mg maintenance doses given every 12 h for five doses. The mean terminal half-life ranged from 29 h to 56 h. Gavestinel was extensively bound to plasma protein (median percentage free <0.01). During gavestinel administration, some patients exhibited elevated levels of bilirubin, which may be the result of shared mechanisms of elimination (glucuronide conjugation and excretion in bile).[2] |
| Synonyms | GV 150526A, Gavestinel sodium salt |
| Molecular Weight | 397.19 |
| Formula | C18H11Cl2N2NaO3 |
| Cas No. | 153436-38-5 |
| Smiles | O=C(NC1=CC=CC=C1)/C=C/C2=C(C([O-])=O)NC3=CC(Cl)=CC(Cl)=C23.[Na+] |
| Relative Density. | no data available |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 90 mg/mL (226.59 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (8.31 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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