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  3. Nelonemdaz

Nelonemdaz (Synonyms: Salfaprodil free base; Neu2000)

目录号: HY-106408 纯度: 99.61%
产品使用指南

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。

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Nelonemdaz Chemical Structure

Nelonemdaz Chemical Structure

CAS No. : 640290-67-1

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥2110
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1 mg ¥800
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5 mg ¥2500
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10 mg ¥4500
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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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[1][2].

IC50 & Target

NMDA receptor[1]

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[1].
Nelonemdazl (10-500 μM) inhibits the electrophysiologic response of cultured cortical neurons to 300 μM NMDA in a concentration-dependent manner[1].
Nelonemdaz (0.1-1 μM) produces a marked reduction of Fe2+-induced neurotoxicity, even at doses of 0.1 to 0.3 μM[1].
Nelonemdaz (0.1-1 μM) blocks the degeneration of neurons and glia in cortical cell cultures[1].
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)[3].
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[3].
Nelonemdaz (0.19-12.5 μM) inhibits malondialdehyde (MDA) formation with an IC50 of 2.72±0.26 μM[3].
Nelonemdaz (0-125 μM) effectively reduces iron-ascorbate-induced lipid peroxidation (IC50=24.56±0.07 μM)[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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[1].
Nelonemdaz (5 mg/kg; i.v.) protects white matter such as axons and myelin as well as gray matter from ischemic brain injury[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Sprague-Dawley rats (260 to 300 g) (clip occlusion model)[1]
Dosage: 0.5-20 mg/kg
Administration: I.v. administration 5 mins after reperfusion
Result: Produced a large neuroprotective effect, with a maximal reduction in infarct volume of 66% at doses of 2.5 to 5 mg/kg.
Not observed neuronal damage in the most vulnerable cortical area after administration of 5 mg/kg.
Animal Model: Male Sprague-Dawley rats (260 to 300 g) (intraluminal thread occlusion model)[1]
Dosage: 5 mg/kg
Administration: I.v. administration 30 mins after reperfusion
Result: Did not change physiologic variables such as arterial pH, PCO2, PO2, and hematocrit.
Reduced infarct volume evolving in the cortex and the striatum substantially.
Reduced white matter damage in the striatum and external capsule markedly.
分子量

383.22

Formula

C15H8F7NO3

CAS 号
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
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 112.5 mg/mL (293.57 mM)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.6095 mL 13.0473 mL 26.0947 mL
5 mM 0.5219 mL 2.6095 mL 5.2189 mL
10 mM 0.2609 mL 1.3047 mL 2.6095 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

参考文献

纯度: 99.61%

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Nelonemdaz
目录号:
HY-106408
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