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Gavestinel

Catalog No. T22798 CAS 153436-38-5

Synonyms: GV 150526, Gavestinel sodium salt

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.

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Gavestinel, CAS 153436-38-5

Pack Size	Availability	Price/USD
1 mg	In stock	$ 38.00
5 mg	In stock	$ 89.00
10 mg	In stock	$ 147.00
25 mg	In stock	$ 248.00
50 mg	In stock	$ 369.00
100 mg	In stock	$ 543.00

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Purity: 99.04%

Biological Description

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Storage & Solubility Information

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 150526, Gavestinel sodium salt
Molecular Weight	398.2
Formula	C18H12Cl2N2NaO3
CAS No.	153436-38-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 90.0 mg/mL (226.6 mM), Sonication is recommended.

References and Literature

1. Di Fabio R, et al. Substituted indole-2-carboxylates as in vivo potent antagonists acting as the strychnine-insensitive glycine binding site. J Med Chem. 1997;40(6):841-850. 2. Hoke JF, et al. Pharmacokinetics of a glycine site antagonist (gavestinel) following multiple dosing in patients with acute stroke. Eur J Clin Pharmacol. 2000;55(11-12):867-872. 3. Lees KR, et al. Glycine antagonist (gavestinel) in neuroprotection (GAIN International) in patients with acute stroke: a randomised controlled trial. GAIN International Investigators. Lancet. 2000;355(9219):1949-1954. 4. Haley EC Jr, et al. Gavestinel does not improve outcome after acute intracerebral hemorrhage: an analysis from the GAIN International and GAIN Americas studies. Stroke. 2005;36(5):1006-1010.

Related compound libraries

This product is contained In the following compound libraries：

Membrane Protein-targeted Compound Library Anti-Neurodegenerative Disease Compound Library Bioactive Compounds Library Max Bioactive Compound Library Neuronal Signaling Compound Library

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Keywords

Gavestinel 153436-38-5 Membrane transporter/Ion channel Neuroscience iGluR NMDAR Gavestinel sodium GV-150526 GV 150526 Gavestinel sodium salt GV150526 inhibitor inhibit

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