Trofinetide (NNZ-2566)
(Synonyms: NNZ-2566) 目录号 : GC30804Trofinetide (NNZ-2566) (NNZ-2566) 是内源性 N 末端三肽 Glycine-Proline-Glutamate (GPE) 的合成类似物,已被证明在脑损伤动物模型中具有神经保护作用。
Cas No.:853400-76-7
Sample solution is provided at 25 µL, 10mM.
Trofinetide, a synthetic analogue of the endogenous N-terminus tripeptide, Glycine-Proline-Glutamate (GPE), has been shown to be neuroprotective in animal models of brain injury.
Trofinetide (NNZ-2566) suppresses penetrating ballistic-like brain injury (PBBI) induced inflammatory cell infiltration at 3 days following PBBI as compare to vehicle treatment. Trofinetide treatment significantly reduces the elevation of IL-6 (79%), E-selectin (81%), IL-1β (76%) and TNF-α (72%) mRNA levels in the injured hemisphere at 12 h post-PBBI, with maximal inhibition occurring between 12 h and 24 h. Trofinetide treatment does not affect the PBBI-induced up-regulation of IL-6 expression at any time point, but does produce significant reductions in the injury-induced up-regulation of IL-1β, INF-γ, and TNF-α expression. Trofinetide treatment suppresses IL-1β expression in the injured brain hemisphere for up to 7 days post-PBBI[1]. The high doses of Trofinetide (NNZ-2566) (10 and 100 mg/kg bolus followed by continuous infusion) attenuate non-convulsive seizure (NCS) occurring beyond 2 h after permanent middle cerebral artery occlusion (pMCAo). All doses of Trofinetide completely suppress the delayed occurrence of NCS as compare with the vehicle-treated animals[2].
[1]. Wei HH, et al. NNZ-2566 treatment inhibits neuroinflammation and pro-inflammatory cytokine expression induced by experimental penetrating ballistic-like brain injury in rats. J Neuroinflammation. 2009 Aug 5;6:19. [2]. Lu XC, et al. NNZ-2566, a glypromate analog, attenuates brain ischemia-induced non-convulsive seizures in rats. J Cereb Blood Flow Metab. 2009 Dec;29(12):1924-32.
Animal experiment: | Three groups of eight rats are evaluated: vehicle/sham, vehicle/penetrating ballistic-like brain injury (PBBI), Trofinetide (NNZ-2566)/PBBI. A bolus injection of 10 mg/kg Trofinetide or 1 mL/kg saline (vehicle) is administered intravenously (IV) to each animal at 30 minutes post-PBBI surgery, immediately followed by a continuous IV infusion of Trofinetide at a rate of 3 mg/kg/h or an equal volume of vehicle for various durations (1 h, 4 h, or 12 h). Rats are subsequently euthanized and brain tissues are collected for processing at 1 h, 4 h, 12 h, 24 h, 3, and 7 days following the initiation of treatment[1]. |
References: [1]. Wei HH, et al. NNZ-2566 treatment inhibits neuroinflammation and pro-inflammatory cytokine expression induced by experimental penetrating ballistic-like brain injury in rats. J Neuroinflammation. 2009 Aug 5;6:19. |
Cas No. | 853400-76-7 | SDF | |
别名 | NNZ-2566 | ||
Canonical SMILES | O=C(O)CC[C@@H](C(O)=O)NC([C@@]1(C)N(C(CN)=O)CCC1)=O | ||
分子式 | C13H21N3O6 | 分子量 | 315.32 |
溶解度 | Water : ≥ 50 mg/mL (158.57 mM) | 储存条件 | Store at -20°C |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 3.1714 mL | 15.8569 mL | 31.7138 mL |
5 mM | 0.6343 mL | 3.1714 mL | 6.3428 mL |
10 mM | 0.3171 mL | 1.5857 mL | 3.1714 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度: mg/ml;
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2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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