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经验公式(希尔记法):
C22H30Cl2N2O4S
化学文摘社编号:
分子量:
489.46
MDL number:
NACRES:
NA.77
UNSPSC Code:
12352200
Quality Level
assay
≥98% (HPLC)
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
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
GluN2B NMDA Receptor
Reversible: yes
Packaging
Packaged under inert gas
Preparation Note
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.
Tahirovic, Y., et al. 2008. J. Med. Chem.51, 5506.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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