Nelonemdaz

(Synonyms: Salfaprodil free base; Neu2000)
目录号: PL01566 纯度: ≥99%
Nelonemdaz (Salfaprodil free base) 是一种 NR2B 选择性和非竞争性的 N- 甲基 -D- 天冬氨酸 (NMDA) 受体拮抗剂,也是一种自由基清除剂。Nelonemdaz 对 NMDA 和自由基诱导的细胞死亡具有出色的神经保护作用。
CAS No. :640290-67-1
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中文名称
Nelonemdaz
英文名称
Nelonemdaz
英文别名
2-Hydroxy-5-[[[2,3,5,6-tetrafluoro-4-(trifluoromethyl)phenyl]methyl]amino]benzoic acid;Nelonemdaz;Neu 2000
Cas No.
640290-67-1
分子式
C15H8F7NO3
分子量
383.22
包装储存
Powder -20°C 3 years;4°C 2 years
详情描述
Nelonemdaz (Salfaprodil free base) 是一种 NR2B 选择性和非竞争性的 N- 甲基 -D- 天冬氨酸 (NMDA) 受体拮抗剂,也是一种自由基清除剂。Nelonemdaz 对 NMDA 和自由基诱导的细胞死亡具有出色的神经保护作用。
产品详情
Nelonemdaz (Salfaprodil free base) 是一种 NR2B 选择性和非竞争性的 N- 甲基 -D- 天冬氨酸 (NMDA) 受体拮抗剂,也是一种自由基清除剂。Nelonemdaz 对 NMDA 和自由基诱导的细胞死亡具有出色的神经保护作用。
生物活性
Nelonemdaz (Salfaprodil free base) is an NR2B-selective and uncompetitive antagonist of N-methyl-D-aspartate (NMDA). Nelonemdaz is also a free radical scavenger. Nelonemdaz has excellent neuroprotection against NMDA- and free radical-induced cell death.
性状
Solid
IC50 & Target[1][2]
NMDA receptor
体外研究(In Vitro)
Nelonemdaz (10-300 μM) shows apparent neuroprotection against 300 μM N-methyl-d-aspartate (NMDA) at doses as low as 30 μM.
Nelonemdazl (10-500 μM) inhibits the electrophysiologic response of cultured cortical neurons to 300 μM NMDA in a concentration-dependent manner.
Nelonemdaz (0.1-1 μM) produces a marked reduction of Fe-induced neurotoxicity, even at doses of 0.1 to 0.3 μM.
Nelonemdaz (0.1-1 μM) blocks the degeneration of neurons and glia in cortical cell cultures.
Nelonemdaz (0-350 μM) effectively scavenges superoxide radicals (IC50=63.07±1.44 μM), nitric oxide (IC50=155.8±4.88 μM), and hydroxyl radicals (IC50=58.45±1.74 μM).
Nelonemdaz (0.78-12.5 μM) decreases the amount of antimycin A-induced ROS/RNS formation in a dose-dependent manner, with an IC50 of 2.21±0.11 μM.
Nelonemdaz (0.19-12.5 μM) inhibits ma
体内研究(In Vivo)
Nelonemdaz (0.5-20 mg/kg; i.v.) reduces cerebral infarct evolving 24 h after 60-mins occlusion of the middle cerebral artery occlusion (MCAO) substantially and dose dependently.
Nelonemdaz (5 mg/kg; i.v.) protects white matter such as axons and myelin as well as gray matter from ischemic brain injury.
has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Gwag BJ, et al. Marked prevention of ischemic brain injury by Neu2000, an NMDA antagonist and antioxidant derived from aspirin and sulfasalazine. J Cereb Blood Flow Metab. 2007 Jun;27(6):1142-51.
[2]. Sung IC, et, al. Neu2000, an NR2B-selective, Moderate NMDA Receptor Antagonist and Potent Spin Trapping Molecule for Stroke. Drug News Perspect. 2010 Nov; 23(9): 549-56.
溶解度数据
In Vitro: DMSO : ≥ 112.5 mg/mL (293.57 mM)配制储备液
搜索质检报告(COA)
[1]. Gwag BJ, et al. Marked prevention of ischemic brain injury by Neu2000, an NMDA antagonist and antioxidant derived from aspirin and sulfasalazine. J Cereb Blood Flow Metab. 2007 Jun;27(6):1142-51.
[2]. Sung IC, et, al. Neu2000, an NR2B-selective, Moderate NMDA Receptor Antagonist and Potent Spin Trapping Molecule for Stroke. Drug News Perspect. 2010 Nov; 23(9): 549-56.

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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