Tat-NR2B9c is a 20-aa peptide, it acts as a postsynaptic density-95 (PSD-95) inhibitor with EC50 of 6.7 nM for PSD-95d2. Tat-NR2B9c also reduces NMDA-induced p38 activation, and possesses neuroprotective efficacy. 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. In male C57BL/6 mice, Tat-NR2B9c (10 nM/g; i.v.) reduces infarction volume , but has no effect at 3 nM/g.
| Cell Experiment | |
|---|---|
| Cell lines | Postnatal mono-cultured WT and YAC128 striatal neurons |
| Preparation method | Postnatal mono-cultured WT and YAC128 striatal neurons are pretreated for 1 h with 200 nM Tat-NR2B9c, and/or SB-239063 (p38 inhibitor), and/or SP-600125 (JNK inhibitor), then incubated with or without 500 μM NMDA for 10 min. After NMDA treatment, striatal neurons are washed once with warm plating medium (PM) and then incubated in conditioned PM (without Tat peptides or p38, JNK inhibitors) for 24 h. Then cells are washed with PBS once and fixed with 4% paraformaldehyde (PFA) for 30 min. |
| Concentrations | 200 nM |
| Incubation time | 1 h |
| Animal Experiment | |
|---|---|
| Animal models | Mice |
| Formulation | - |
| Dosages | 0.0, 3.0, 10.0 nMole/g |
| Administration | intravenously via the tail vein using a pump in a volume of 1 µL/g |
| Molecular Weight | 2518.88 |
| Formula | C105H188N42O30 |
| CAS Number | 500992-11-0 |
| Solubility (25°C) | Water 30 mg/mL |
| Storage | -20°C, sealed |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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