| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 100mg |
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| 250mg | |||
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| Targets |
Gavestinel Sodium targets the glycine site on the NMDA receptor, acting as a non-competitive antagonist. It binds to an allosteric site distinct from the glutamate or glycine binding domains. This noncompetitive mechanism results in sustained receptor blockade, even in the presence of high glutamate concentrations. It displays >1000-fold selectivity over NMDA, AMPA, and kainate binding sites.
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| ln Vitro |
In vitro, gavestinel sodium binds to the glycine site of the NMDA receptor with a pKi of 8.5. It is a selective, non-competitive antagonist of the NMDA receptor. Its binding affinity and selectivity have been confirmed in radioligand binding assays. It displays >1000-fold selectivity over other glutamate receptor binding sites.
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| ln Vivo |
In vivo, gavestinel sodium has been studied for acute ischemic stroke research. It has oral activity. Its noncompetitive NMDA receptor antagonism provides neuroprotection by blocking excessive glutamate signaling without interfering with normal glutamatergic transmission. Its efficacy has been evaluated in preclinical models.
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| Enzyme Assay |
Cell-free assays for gavestinel sodium are radioligand binding assays using membrane preparations from brain tissue or cells expressing NMDA receptors. The compound's binding affinity (pKi) is determined by its ability to displace a labeled glycine site ligand such as [3H]glycine. Its molecular weight (397.19) is confirmed by mass spectrometry.
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| Cell Assay |
Cellular assays for gavestinel sodium are performed using neuronal cell cultures or cells expressing NMDA receptors. Cells are treated with varying concentrations of gavestinel sodium, and NMDA receptor-mediated calcium influx or currents are measured using calcium imaging or patch-clamp electrophysiology. Its noncompetitive antagonist activity is confirmed.
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| Animal Protocol |
In vivo animal experiments for gavestinel sodium are conducted in animal models of ischemic stroke, such as middle cerebral artery occlusion (MCAO) models. Animals are administered gavestinel sodium orally or intravenously, and infarct size, neurological deficit scores, and survival are assessed. Its neuroprotective efficacy is evaluated.
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| ADME/Pharmacokinetics |
Gavestinel Sodium has a molecular weight of 397.19 g/mol and a molecular formula of C18H14ClN2NaO4 (for the sodium salt). It has a purity of ≥98%. It is soluble in DMSO and should be stored under recommended conditions. Its chemical name is not specified in the available sources.
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| Toxicity/Toxicokinetics |
The toxicological profile of gavestinel sodium has been evaluated in preclinical studies. As an NMDA receptor antagonist, it may have effects on cognition and motor function. No significant toxicity has been reported. Its safety has been studied in clinical trials for acute ischemic stroke.
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| References | |
| Additional Infomation |
A highly effective and selective non-competitive antagonist that acts on the glycine binding site (Kd = 0.8 nM) in the NMDA receptor channel complex, which is insensitive to strychnine. Gavestinel exhibits more than 1000 times higher selectivity for NMDA, AMPA, and fucoidine binding sites than these, and has high oral bioavailability and strong in vivo activity.
Gavestinel Sodium is a potent, selective, and non-competitive NMDA receptor antagonist that binds to the glycine site. It is also known as GV 150526A. It has been studied for acute ischemic stroke research. It is a research compound and is not approved for clinical use. |
| Molecular Formula |
C18H11N2O3CL2-.NA+
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|---|---|
| Molecular Weight |
397.18734
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| Exact Mass |
396.004
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| CAS # |
153436-38-5
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| Related CAS # |
Gavestinel;153436-22-7
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| PubChem CID |
16759177
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| Appearance |
White to light yellow solid powder
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| LogP |
5.346
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
26
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| Complexity |
543
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC=C(C=C1)NC(=O)/C=C/C2=C(NC3=C2C(=CC(=C3)Cl)Cl)C(=O)[O-].[Na+]
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| InChi Key |
GRSDSTMFQHAESM-UHDJGPCESA-M
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| InChi Code |
InChI=1S/C18H12Cl2N2O3.Na/c19-10-8-13(20)16-12(17(18(24)25)22-14(16)9-10)6-7-15(23)21-11-4-2-1-3-5-11;/h1-9,22H,(H,21,23)(H,24,25);/q;+1/p-1/b7-6+;
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| Chemical Name |
sodium;3-[(E)-3-anilino-3-oxoprop-1-enyl]-4,6-dichloro-1H-indole-2-carboxylate
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 : ~100 mg/mL (~251.77 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.29 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.29 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.29 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5177 mL | 12.5884 mL | 25.1769 mL | |
| 5 mM | 0.5035 mL | 2.5177 mL | 5.0354 mL | |
| 10 mM | 0.2518 mL | 1.2588 mL | 2.5177 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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