Tat-NR2B9c TFA (Tat-NR2Bct TFA) is a postsynaptic density-95 (PSD-95) inhibitor, with EC 50 values of 6.7 nM and 670 nM for PSD-95d2 (PSD-95 PDZ domain 2) and PSD-95d1, respectively. Tat-NR2B9c TFA disrupts the PSD-95/NMDAR interaction, inhibiting NR2A and NR2B binding to PSD-95 with IC 50 values of 0.5 μM and 8 μM, respectively. Tat-NR2B9c TFA also inhibits neuronal nitric oxide synthase (nNOS)/PSD-95 interaction, and possesses neuroprotective efficacy In Vitro Tat-NR2B9c is a PSD-95 inhibitor, with an EC 50 of 6.7 nM for PSD-95d2, representing a >100-fold higher affinity for this domain than for PSD-95d1 (EC 50 , 0.67 μM). Tat-NR2B9c inhibits NMDAR2A, NMDAR2B, and NMDAR2C binding to PSD-95, with IC 50 s of 0.5 μM, ∼8 μM, and 0.75 μM, respectively. Tat-NR2B9c also blocks the interaction between PSD-95 and nNOS with an IC 50 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo Tat-NR2B9c (10 nmol/g, i.v.) reduces infarction volume of male C57BL/6 mice, but has no effect at 3 nmol/g. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:NMDA Receptor nNOS
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Tat-NR2B9c TFA
CAS number:1834571-04-8 molecular formula:C105H188N42O30
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| Chinese alias | Tat-NR2B9c 三氟乙酸 | ||
| English alias | UNII-D45TI2TWMA | Nerinetide | Tat NR2B9c | AKOS040740169 | L-Valine, L-tyrosylglycyl-L-arginyl-L-lysyl-L-lysyl-L-arginyl-L-arginyl-L- glutaminyl-L-arginyl-L-arginyl-L-arginyl-L-lysyl-L-leucyl-L-seryl-L-seryl-L-isoleucyl-L-alpha-glutamyl-L-seryl-L-alpha-a | ||
| CAS number | 1834571-04-8 | molecular formula | C105H188N42O30 |
| molecular weight | 2518.9 g/mol | Exact mass | ≥99% |
| PSA | 1260.000 Ų | logp | -19.300 |
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