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Nelonemdaz

Nelonemdaz

产品编号 T16286   CAS 640290-67-1
别名: Neu2000

Neu2000 is an uncompetitive antagonist of N-methyl-D-aspartate (NMDA) receptor.

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Nelonemdaz Chemical Structure
Nelonemdaz, CAS 640290-67-1
规格 价格/CNY 货期 数量
1 mg ¥ 662 现货
5 mg ¥ 1,980 现货
10 mg ¥ 3,730 现货
25 mg ¥ 5,930 现货
50 mg ¥ 7,850 现货
100 mg ¥ 10,800 现货
500 mg ¥ 21,600 现货
1 mL * 10 mM (in DMSO) ¥ 1,730 现货
其他形式的 Nelonemdaz:
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
产品目录号及名称: Nelonemdaz (T16286)
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纯度: 98.95%
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生物活性
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存储 & 溶解度
参考文献
产品描述 Neu2000 is an uncompetitive antagonist of N-methyl-D-aspartate (NMDA) receptor.
体外活性 Neu2000 displays apparent neuroprotection against 300 μM N-methyl-D-aspartate (NMDA) at doses as low as 30 μM. Neu2000 inhibits the electrophysiologic response of cultured cortical neurons to 300 μM NMDA in a concentration-dependent manner, indicating that the effect is mediated by a specific action at NMDA receptors. Neu2000 does not protect cortical neurons against α-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid- or kainate-mediates excitotoxicity. Neu2000 (100 μM) obviously decreases the maximal NMDA response by 58.31±2.72% (n=5) and the EC50 values of NMDA from 18.88±1.85 to 9.92±0.17 μM (n=5, P<0.05). The Neu2000 dose-response has an IC50 of 35.38±5.94 μM and Hill's coefficient of 0.91 (n=8) [1].
体内活性 Pharmacokinetic analysis reveals that the half-life of Neu2000 is 1.42, 2.14, and 1.79?h following intraperitoneal administration of 10, 25, and 50?mg/kg, respectively. The results of the blood-brain barrier (BBB) test also reveals significant changes in open field locomotion in spinal cord-injured animals treated with Neu2000 compare to vehicle-treated animals. Single (p<0.05) or repeated (p<0.01) Neu2000 treatment causes a decreased swing to stance ratio to compare to vehicle-treated animals. Repeated treatment with Neu2000 induces a 45.6% decrease (p<0.01) in overall lesion volume compared to vehicle treatment, while a single administration of Neu2000 results in a 36.8% decrease (p<0.05) in overall lesion volume. Compare to sham controls, the levels of basal mitochondrial ROS are obviously elevated at 24?h post-surgery in both the vehicle-treated (4.1-fold, p<0.01) and Neu2000-treated (2.9-fold, p<0.01) groups. The Cmax (maximum plasma concentration) is calculated as 3.86, 18.73, and 52.83?μg/mL and the AUC (area under the curve) is determined to be 7.37, 55.15, and 96.77?μg/h/mL at the same respective doses [2].
别名 Neu2000
分子量 383.22
分子式 C15H8F7NO3
CAS No. 640290-67-1

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 112.5 mg/mL (293.57 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6095 mL 13.0473 mL 26.0947 mL 65.2367 mL
5 mM 0.5219 mL 2.6095 mL 5.2189 mL 13.0473 mL
10 mM 0.2609 mL 1.3047 mL 2.6095 mL 6.5237 mL
20 mM 0.1305 mL 0.6524 mL 1.3047 mL 3.2618 mL
50 mM 0.0522 mL 0.2609 mL 0.5219 mL 1.3047 mL
100 mM 0.0261 mL 0.1305 mL 0.2609 mL 0.6524 mL

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TargetMol Library Books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. Springer JE, et al. The functional and neuroprotective actions of Neu2000, a dual-acting pharmacological agent, in the treatment of acute spinal cord injury. J Neurotrauma. 2010 Jan;27(1):139-49.
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母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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Keywords

Nelonemdaz 640290-67-1 DNA Damage/DNA Repair Topoisomerase Neu2000 Inhibitor inhibitor inhibit

 

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