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Trofinetide (NNZ-2566) Sale

(Synonyms: NNZ-2566) 目录号 : GC30804

Trofinetide (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。

Trofinetide (NNZ-2566) Chemical Structure

Cas No.:853400-76-7

规格 价格 库存 购买数量
5mg
¥1,440.00
现货
10mg
¥2,340.00
现货
25mg
¥4,320.00
现货

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Sample solution is provided at 25 µL, 10mM.

Description

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.

实验参考方法

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.
[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.

化学性质

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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溶解性数据

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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
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