Nelonemdaz potassium - CAS:916214-57-8

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Nelonemdaz potassium (Synonyms:Salfaprodil; Neu2000 potassium)

目录号 : KM9186 CAS No. : 916214-57-8 纯度 : 98%

Data Sheet 产品使用指南

Nelonemdaz (Salfaprodil) potassium 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 potassium 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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生物活性

Nelonemdaz (Salfaprodil) potassium is an NR2B-selective and uncompetitive antagonist of N-methyl-D-aspartate (NMDA). Nelonemdaz potassium is also a free radical scavenger. Nelonemdaz potassium has excellent neuroprotection against NMDA- and free radical-induced cell death.

体外研究

Nelonemdaz potassium (10-300 μM) shows apparent neuroprotection against 300 μM N-methyl-d-aspartate (NMDA) at doses as low as 30 μM.
Nelonemdaz potassium (10-500 μM) inhibits the electrophysiologic response of cultured cortical neurons to 300 μM NMDA in a concentration-dependent manner.
Nelonemdaz potassium (0.1-1 μM) produces a marked reduction of Fe-induced neurotoxicity, even at doses of 0.1 to 0.3 μM.
Nelonemdaz potassium (0.1-1 μM) blocks the degeneration of neurons and glia in cortical cell cultures.
Nelonemdaz potassium (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 potassium (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 potassium (0.19-12.5 μM) inhibits malondialdehyde (MDA) formation with an IC₅₀ of 2.72±0.26 μM.
Nelonemdaz potassium (0-125 μM) effectively reduces iron-ascorbate-induced lipid peroxidation (IC₅₀=24.56±0.07 μM).

体内研究

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

Animal Model:	Male Sprague-Dawley rats (260 to 300 g) (clip occlusion model)
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)
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.

分子式

C₁₅H₇F₇KNO₃

分子量

421.31

CAS号

916214-57-8

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 : 200 mg/mL (474.71 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.3735 mL	11.8677 mL	23.7355 mL
5 mM	0.4747 mL	2.3735 mL	4.7471 mL
10 mM	0.2374 mL	1.1868 mL	2.3735 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。

纯度： 98%

Data Sheet

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