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GluN2B-NMDAR antagonist-2 (compound S-58) is an effective and selective NMDAR-GluN2B antagonist that can cross the blood-brain barrier, with an IC50 value of 74.01 nM. It exhibits mild cytotoxicity and reduces both infarct size and neurological deficit scores in the brain, indicating its potential for stroke research.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
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| 10 mg | Inquiry | Inquiry | Inquiry | |
| 50 mg | Inquiry | Inquiry | Inquiry |
| Description | GluN2B-NMDAR antagonist-2 (compound S-58) is an effective and selective NMDAR-GluN2B antagonist that can cross the blood-brain barrier, with an IC50 value of 74.01 nM. It exhibits mild cytotoxicity and reduces both infarct size and neurological deficit scores in the brain, indicating its potential for stroke research. |
| Targets&IC50 | GluN2B:74.01 nM |
| In vitro | GluN2B-NMDAR antagonist-2 (compound S-58) (1, 3, 10 µM) does not significantly extend the action potential duration (APD90) in hiPSC-CM. When administered at concentrations ranging from 0 to 300 µM over 48 hours, it exhibits slight cytotoxicity to primary mouse neurons, VERO, L929, and HEK293 cells. |
| In vivo | The compound GluN2B-NMDAR antagonist-2, when administered intravenously at doses of 5, 10, and 20 mg/kg, reduces cerebral infarction rates and neurological deficit scores in a dose-dependent manner in the MCAO rat model. In ICR mice, GluN2B-NMDAR antagonist-2 (450, 900 mg/kg; i.v.) demonstrates favorable safety, with a maximum tolerated dose (MTD) of 450 mg/kg. |
| Formula | C24H25Cl2N3O3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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