生物活性
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.
化学数据
| 分子量 | 2518.88 |
| 分子式 | C105H188N42O30 |
| CAS号 | 500992-11-0 |
| 纯度 | >98% |
| 溶解性（25°C） | Water 30 mg/mL |
| 储存和运输条件 | -20°C, sealed
常温运输及临时存放 |
实验操作 来自于公开的文献，仅供相同实验参考（如实验材料、目的不同，请参考其他文献）
| 细胞实验 |
|---|
| 细胞系 | Postnatal mono-cultured WT and YAC128 striatal neurons |
| 方法 | 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. |
| 浓度 | 200 nM |
| 处理时间 | 1 h |
| 动物实验 |
|---|
| 动物模型 | Mice |
| 配制 | - |
| 剂量 | 0.0, 3.0, 10.0 nMole/g |
| 给药处理 | intravenously via the tail vein using a pump in a volume of 1 μL/g |
不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）
| 小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 |
| 重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| 体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km系数 | 3 | 6 | 12 | 8 | 5 | 20 |
| 动物 A (mg/kg) = 动物 B (mg/kg) × | 动物 B的Km系数 |
| 动物 A的Km系数 |
例如，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。
储备液配制
以下数据基于产品分子量，对于特殊产品，请参照COA中的储备液配制条件和说明进行操作。
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 0.397 mL | 1.985 mL | 3.97 mL |
| 5 mM | 0.0794 mL | 0.397 mL | 0.794 mL |
| 10 mM | 0.0397 mL | 0.1985 mL | 0.397 mL |
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