产品
编 号:F370489
分子式:C105H188N42O30
分子量:2518.88
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1mg
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5mg
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10mg
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询价
25mg
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生物活性:
Tat-NR2B9c (Tat-NR2Bct; NA-1) is a postsynaptic density-95 (PSD-95) inhibitor, with EC50 values of 6.7 nM and 670 nM for PSD-95d2 (PSD-95 PDZ domain 2) and PSD-95d1, respectively. Tat-NR2B9c disrupts the PSD-95/NMDAR interaction, inhibiting NR2A and NR2B binding to PSD-95 with IC50 values of 0.5 μM and 8 μM, respectively. Tat-NR2B9c also inhibits?neuronal nitric oxide synthase (nNOS)/PSD-95?interaction, and possesses neuroprotective efficacy.

体内研究:
Tat-NR2B9c (10?nmol/g, i.v.) reduces infarction volume of male C57BL/6 mice, but has no effect at 3?nM/g.

体外研究:
Tat-NR2B9c is a PSD-95 inhibitor, with an EC50 of 6.7 nM for PSD-95d2, representing a >100-fold higher affinity for this domain than for PSD-95d1 (EC50, 0.67 μM). Tat-NR2B9c inhibits NMDAR2A, NMDAR2B, and NMDAR2C binding to PSD-95, with IC50s of 0.5 μM, ~8 μM, and 0.75 μM, respectively.Tat-NR2B9c also blocks the interaction between PSD-95 and nNOS with an IC50 of ~0.2 μM. Tat-NR2B9c reduces association of PSD-95 with GluN2B by ~50% in the YAC128 striatum, decreases NMDA-induced p38 activation in YAC128 striatal tissue, but shows no effect on the NMDA-induced JNK activation.
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