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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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Gavestinel sodium

Key Properties

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CAS Number153436-38-5
MW397.19
Purity99.04% (May vary between batches)
FormulaC18H11Cl2N2NaO3
SMILESO=C(NC1=CC=CC=C1)/C=C/C2=C(C([O-])=O)NC3=CC(Cl)=CC(Cl)=C23.[Na+]
TargetNMDAR,iGluR
SolubilityDMSO: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-20°C
Expiration Date12 months from date of receipt.
DisclaimerFor 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
Quality Guarantee

Quality Guarantee

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Compound Identifiers

PubChem CID
16759177 ↗

Key Properties

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No computed properties available.

Protocol Information

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Available Sizes

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1 mg
$ 80.00
5 mg
$ 130.00
10 mg
$ 190.00
25 mg
$ 290.00
50 mg
$ 410.00
100 mg
$ 590.00
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