| 产品描述: | NAB-14 is a potent, selective, orally active and non-competitive GluN2C/2D antagonists with an IC50 of 580 nM for GluN1/GluN2D. NAB-14 shows >800-fold selective for recombinant GluN2C and GluN2D over GluN2A and GluN2B. NAB-14 can cross the blood-brain-barrier. |
| 体外研究: |
NAB-14 (20 mg/kg; p.o.) shows high systemic exposure with peak brain free of 3.2 and 3.8 nM for mouse and rat, respectively. |
| 体内研究: |
NAB-14 (compound 14) shows inhibition with IC50s of 15 µM and 5.1 µM for GluN1/2AC1/2CC2 and GluN1/2AC1/2CC2 receptors, respectively. NAB-14 (20 µM; 24 h) inhibits native GluN2D-containing receptors in brain slices with no effect on native GluN2A- or GluN2B-containing NMDARs in cultures cortical neurons. NAB-14 (10 µM) reduces the peak amplitude of evoked EPSCs to 55 ± 3.0%, and significantly reduced the τW of EPSC deactivation. NAB-14 (10 µM) decreases the peak amplitude and charge transfer of interneuron EPSCs to 59 ± 9.9% and 63 ± 9.7%, respectively. And NAB-14 decreases τW for interneuron EPSCs from 150 ± 12 ms to 101 ± 14 ms. |
| 保存条件: |
-80°C 6个月;-20°C 1个月 |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.846 ml |
14.229 ml |
28.458 ml |
| 5 mM |
0.569 ml |
2.846 ml |
5.692 ml |
| 10 mM |
0.285 ml |
1.423 ml |
2.846 ml |
| 50 mM |
0.057 ml |
0.285 ml |
0.569 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |