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
Molecular Weight: 489.46. Empirical Formula: C22H30Cl2N2O4S. Assay: ≥. 98% (HPLC). Quality Level: 100. form: solid (sticky). potency: 0.19 . μ. M 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. Storage Class Code: 11 - Combustible Solids. WGK: WGK 3. Flash Point(F): Not applicable. Flash Point(C): Not applicable.- UPC:
- 51143015
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 5380960001
