5.38096

GluN2B NMDA Receptor Antagonist, 93-31

• Synonym(s): GluN2B NMDA Receptor Antagonist, 93-31, (S)-N-(4-(3-(butyl(3,4-dichlorophenethyl)amino)-2-hydroxypropoxy)phenyl)methanesulfonamide
• Empirical Formula (Hill Notation): C₂₂H₃₀Cl₂N₂O₄S
• CAS Number: 457897-98-2
• Molecular Weight: 489.46
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Assay: ≥98% (HPLC)
• Quality Level: 100
• form: solid (sticky)
• potency: 0.19 μM IC₅₀
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: light yellow to yellow
• solubility: DMSO: 100 mg/mL
• storage temp.: −20°C

Description

General description

A tertiary N-alkylamine that acts as a pH dependent antagonist of GluN2B-NMDA receptors. Shown to be about 10-fold more potent in ischemic tissue (pH 6.9) than in normal healthy tissue (pH 7.6) (IC₅₀ = 190 nM and 1.8 µM, respectively). Effectively reduces the infarct volume in damaged brain tissue in a murine model of ischemic stroke (at 10 mg/kg, ED₅₀ ≤ 1 mg/kg) without impairing coordination or motor function. Also displays binding to hERG (IC₅₀ = 70 nM) and alpha1-adrenergic receptor (IC₅₀ = 4.9 µM).

Biochem/physiol Actions

Primary Target
GluN2B NMDA Receptor

Reversible: yes

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Yuan, H., et al. 2015. Neuron.85, 1305.
Tahirovic, Y., et al. 2008. J. Med. Chem.51, 5506.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable