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(-)-Dizocilpine maleate

(-)-Dizocilpine maleate

产品编号 T6352   CAS 121917-57-5
别名: C13737, (-)-MK 801 (Maleate), (-)-MK 801马来酸, (-)-MK 801 Maleate

(-)-Dizocilpine maleate ((-)-MK 801 (Maleate)) 是一种选择性且非竞争性的 N-甲基-D-天冬氨酸 (NMDA) 受体拮抗剂,Ki 为 211.7 nM。它是一种 Dizocilpine 的活性较低的 (-)-对映体,具有抗抑郁作用。

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(-)-Dizocilpine maleate Chemical Structure
(-)-Dizocilpine maleate, CAS 121917-57-5
规格 价格/CNY 货期 数量
5 mg ¥ 239 现货
10 mg ¥ 373 现货
25 mg ¥ 695 现货
50 mg ¥ 1,230 现货
100 mg ¥ 2,090 待询
1 mL * 10 mM (in DMSO) ¥ 415 现货
其他形式的 (-)-Dizocilpine maleate:
产品目录号及名称: (-)-Dizocilpine maleate (T6352)
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纯度: 99.89%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 (-)-Dizocilpine maleate ((-)-MK 801 (Maleate)) is a potent, selective and non-competitive NMDA receptor antagonist with Kd of 37.2 nM in rat brain membranes.
靶点活性 NMEA:Kd:37.2nM
体外活性 Neurophysiological studies in vitro, using a rat cortical-slice preparation, demonstrates a potent, selective, and noncompetitive antagonistic action of dizocilpine on depolarizing responses to N-Me-D-Asp but not to kainate or quisqualate. The potencies of phencyclidine, ketamine, SKF 10047, and the enantiomers of dizocilpine as N-Me-D-Asp antagonists correlate closely (r = 0.99) with their potencies as inhibitors of [3H] dizocilpine binding. This suggests that the dizocilpine binding sites are associated with N-Me-D-Asp receptors and provides an explanation for the mechanism of action of dizocilpine as an anticonvulsant.
体内活性 All the control rats have severe permanent neurological deficits after ischemic spinal cord injury (ISCI), whereas the dizocilpine–treated rats have statistically (P < .05) better neurological outcome and good recovery. Histopathology reveals severe neuronal necrosis in the lumbar gray matter of control rats, whereas dizocilpine–treated rats show mild injury. These results demonstrate that a single dose of dizocilpine given before ISCI provides significant neuroprotection.
激酶实验 In vitro binding assays:For in vitro binding assays, cerebral cortices from male Sprague-Dawley rats (200-300 g) are homogenized in 9 volumes of ice-cold sucrose by nine strokes with a Teflon/glass homogenizer at 500 rpm. The homogenate is centrifuged for 10 min at 1000 x g, and the supernatant is recentrifuged at 10,000 x g for 20 min at 4 ℃. The pellet is suspended in assay buffer and incubated for 20 min prior to final centrifugation at 10,000 x g for 20 min at 4 ℃. The pellet is resuspended in assay buffer (70 ml per gram of original tissue). Binding of [3H] dizocilpine is measured by incubating 750 ul duplicate aliquots of this crude membrane suspension (=0.75 mg of protein) with 100 ul of buffer containing displacer or of buffer alone (total binding), 100 ul of 50 nM [3H] dizocilpine, and 50 ul of buffer for 60 min at 23 ℃. Nonspecific binding is defined by unlabeled dizocilpine. Incubation is terminated by rapid filtration through Whatman GF/B filters, which are washed immediately with two 5-ml portions of ice-cold assay buffer in a Brandel M 24-R cell harvester. The time required for the complete filtration and washing procedure is less than 10 sec. Radioactivity on the filters is determined by liquid scintillation counting in standard vials with 10 ml of Hydrofluor at 41% counting efficiency.
细胞实验 Cell lines: mixed neuronal/glial cell culturesConcentrations: 10 μMIncubation Time: 30 minutesMethod: Primary mixed neuronal/glial cultures are prepared from fetal rat brains. Mature cultures are exposed to dissolved isoflurane [0.4 mM (1.8 minimum alveolar concentration) or 1.6 mM (7 minimum alveolar concentration)] or dizocilpine (10 μM), and NMDA (0 or 3 μM) at 37 ℃ for 30 minutes. Apoptosis is assessed using terminal-deoxy-nucleotidyl end-nick labeling oligonucleosomal DNA fragmentation enzyme-linked immunosorbent assay, and caspases-3 and -9 activation assays.
动物实验 Animal Models: ischemic spinal cord injury medelFormulation: N/ADosages: 1 mg/kgAdministration: IV
别名 C13737, (-)-MK 801 (Maleate), (-)-MK 801马来酸, (-)-MK 801 Maleate
分子量 337.37
分子式 C20H19NO4
CAS No. 121917-57-5

存储

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

溶解度

Ethanol: 7 mg/mL(20.7 mM)

DMSO: 68 mg/mL (201.55 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
Ethanol / DMSO 1 mM 2.9641 mL 14.8205 mL 29.641 mL 74.1026 mL
5 mM 0.5928 mL 2.9641 mL 5.9282 mL 14.8205 mL
10 mM 0.2964 mL 1.4821 mL 2.9641 mL 7.4103 mL
20 mM 0.1482 mL 0.741 mL 1.4821 mL 3.7051 mL
DMSO 50 mM 0.0593 mL 0.2964 mL 0.5928 mL 1.4821 mL
100 mM 0.0296 mL 0.1482 mL 0.2964 mL 0.741 mL

计算器

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参考文献

1. Wong EH, et al. Proc Natl Acad Sci U S A, 1986, 83(18), 7104-7108. 2. Snell LD, et al. Eur J Pharmacol, 1988, 145(2), 223-226.
AMPA receptor modulator-6 cis-PDA Isoxsuprine hydrochloride Procyclidine hydrochloride QNZ46 Orphenadrine hydrochloride 6-Hydroxykynurenic acid NMDAR/TRPM4-IN-2

相关化合物库

该产品包含在如下化合物库中:
神经退行性疾病化合物库 NO PAINS 化合物库 抗阿尔茨海默症化合物库 神经递质受体化合物库 抗帕金森病化合物库 离子通道库 抗癌化合物库 临床前化合物库 经典已知活性库 神经信号分子库

剂量换算

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体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

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。

第一步:请输入动物实验的基本信息
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第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
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技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

(-)-Dizocilpine maleate 121917-57-5 Membrane transporter/Ion channel Neuroscience NMDAR iGluR less-active transporters ()Dizocilpine maleate C 13737 Inhibitor C13737 (-)-MK 801 (Maleate) Dizocilpine inhibit NMDA ( ) Dizocilpine maleate MK-801 Maleate C-13737 (-)-MK 801马来酸 MK801 monoamine Ionotropic glutamate receptors Dizocilpine Maleate (-)-MK 801 Maleate antidepressant MK-801 MK801 Maleate MK 801 MK 801 Maleate inhibitor

 

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