产品
编 号：F086149
分子式：C20H21N3O3
分子量：351.4
分子式：C20H21N3O3
分子量：351.4
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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5mg
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10mg
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25mg
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50mg
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100mg
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结构图
CAS No: 1237541-73-9
产品详情
生物活性：
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.
体内研究：
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.Animal Model:Mice and rats
Dosage:20 mg/kg
Administration:P.o.
Result:Showed high systemic exposure with peak brain free of 3.2 and 3.8 nM for mouse and rat, respectively.
体外研究：
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.
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.
体内研究：
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.Animal Model:Mice and rats
Dosage:20 mg/kg
Administration:P.o.
Result:Showed high systemic exposure with peak brain free of 3.2 and 3.8 nM for mouse and rat, respectively.
体外研究：
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.
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