Gavestinel sodium

SKU: orb1704518

Description

Gavestinel sodium is an orally active, potent, and selective noncompetitive NMDA receptor antagonist targeting the glycine site with a pKi of 8.5. It has been investigated in clinical studies for acute ischemic stroke and is used in research to study excitotoxicity in both in vitro and in vivo models of neurological injury.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Images & Validation

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Key Properties

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CAS Number	153436-38-5
MW	397.19
Purity	99.69%
Formula	C₁₈H₁₁Cl₂N₂NaO₃
SMILES	O=C(NC1=CC=CC=C1)/C=C/C2=C(C([O-])=O)NC3=CC(Cl)=CC(Cl)=C23.[Na+]
Target	NMDAR,iGluR
Solubility	DMSO:90 mg/mL (226.59 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (8.31 mM)

Bioactivity

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Target 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).

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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NMDA receptor, GV 150526, GV 150526A, GV150526, GV-150526, iGluR, Gavestinel, Gavestinel sodium, Gavestinel sodium salt

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Compound Identifiers

PubChem CID

16759177 ↗

Key Properties

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No computed properties available.

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