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Dizocilpine Maleate

产品编号 T3320 CAS 77086-22-7

别名: (+)-Mk-801 Hydrogen Maleate, MK 801, 地卓亚平马来酸盐, Dizocilpine hydrogen maleate, 地佐环平马来酸盐, (+)-MK 801 maleate, (+)-MK 801 (Maleate)

Dizocilpine Maleate (MK 801) 是一种选择性和非竞争性的 NMDA 受体拮抗剂，Kd 值为 37.2 nM。它用于治疗 NMDA 受体可能发挥重要作用的多种神经退行性疾病或疾病。

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Dizocilpine Maleate, CAS 77086-22-7

规格	价格/CNY	货期
5 mg	￥ 198	现货
10 mg	￥ 359	现货
25 mg	￥ 732	现货
50 mg	￥ 1,310	现货
100 mg	￥ 2,080	现货
200 mg	￥ 3,130	现货
1 mL * 10 mM (in DMSO)	￥ 198	现货

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其他形式的 Dizocilpine Maleate:

Dizocilpine
现货
(-)-Dizocilpine maleate
现货

选择批次

纯度: 99.96%

纯度: 99.89%

纯度: 99%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Dizocilpine Maleate (MK 801) is a potent noncompetitive antagonist of the NMDA receptor (RECEPTORS, N-METHYL-D-ASPARTATE) with Kd of 37.2 nM in rat brain membranes. The drug has been considered for the wide variety of neurodegenerative conditions or disorders in which NMDA receptors may play an important role.
靶点活性	NMDAR:37.2 nM(Kd)
体外活性	[3H]MK-801 labels high-affinity binding sites in rat cerebral cortical membranes in a saturable manner. MK-801 produces a potent blockade of depolarizing responses to NMDA in rat cerebral cortical slices. The only compounds that are able to compete for [3H]MK-801 binding sites are substances known to block the responses of excitatory amino acids mediated by the NMDA receptor subtype. [1] MK-801 inhibits N-methyl-D-aspartate-induced [3H]norepinephrine (NE) release and [3H]TCP binding in the hippocampus with IC50 of 20 nM and 9 nM, respectively. [2] MK-801 causes a progressive, long-lasting blockade of current induced by NMDA. Mg2+ (10 mM) prevents MK-801 from blocking the N-Me-D-Asp-induced current, even when MK-801 is applied for a long time in the presence of NMDA. MK-801 is also effective at blocking NMDA-activated single-channel activity in outside-out patches. [3] MK-801 (< 500 μM) prevents LPS-induced activation of microglia in a concentration-dependent manner with increased Cox-2 protein expression in BV-2 cells. MK-801 (< 500 μM) reduces microglial TNF-α output with EC50 of 400 μM in BV-2 cells. [4]
体内活性	Treatment of mice with MK-801 (1 mg/kg) before each METH injection reduced the extent of DA depletion by 55% in striatal of mice. MK-801 (1 mg/kg) attenuates the effects of METH on microglial activation in striatal of mice. [4] MK-801 (0.05 mg/kg or 0.2 mg/kg, i.p.) in rats just prior to reactivation of the cocaine-associated memory in the CPP context attenuates subsequent cocaine-primed reinstatement, while no disruption occurres in rats that do not receive reactivation in the CPP context. MK-801 (0.2 mg/kg, i.p.) prior to two reactivation sessions in the home cage does not suppress subsequent cocaine-primed reinstatement. [5]
激酶实验	Cerebral cortices from male Sprague-Dawley rats (200-300 g) are homogenized in 9 volumes of ice-cold 0.32mol/Lsucrose by nine strokes with a Teflon/glass homogenizer at 500 rpm. The homogenate is centrifuged for 10 min at 1×103 g, and the supernatant is recentrifuged at 1×104 g for 20 min at 4°C. The pellet is suspended in assay buffer (118 mM NaCl/4.7 mM KCl/1.2 mM MgSO4/5 mM NaHCO3/20 mM Hepes/1.2 mM KH2PO4/2.5 mM CaCl2/11 mM glucose, pH 7.4) and incubated at 23°C for 20 min prior to final centrifugation at 1×103 g for 20 min at 4°C. The pellet is resuspended in assay buffer (70 mL per gram of original tissue). Binding of [3H]MK-801 is measured by incubating 750 μL duplicate aliquots of this crude membrane suspension (=0.75 mg of protein) with 100 μL of buffer containing displacer or of buffer alone (total binding), 100 μL of 50 nM [3H]MK-801, and 50 μL of buffer for 60 min at 23°C. Nonspecific binding is defined by 100 μM (final concentration) unlabeled MK-801.

别名	(+)-Mk-801 Hydrogen Maleate, MK 801, 地卓亚平马来酸盐, Dizocilpine hydrogen maleate, 地佐环平马来酸盐, (+)-MK 801 maleate, (+)-MK 801 (Maleate)
分子量	337.38
分子式	C20H19NO4
CAS No.	77086-22-7

存储

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

溶解度

DMSO: 33.7 mg/mL (100 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	2.964 mL	14.8201 mL	29.6402 mL	74.1004 mL
	5 mM	0.5928 mL	2.964 mL	5.928 mL	14.8201 mL
	10 mM	0.2964 mL	1.482 mL	2.964 mL	7.41 mL
	20 mM	0.1482 mL	0.741 mL	1.482 mL	3.705 mL
	50 mM	0.0593 mL	0.2964 mL	0.5928 mL	1.482 mL
	100 mM	0.0296 mL	0.1482 mL	0.2964 mL	0.741 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

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配液浓度

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. 3. Huettner JE, et al. Proc Natl Acad Sci U S A, 1988, 85(4), 1307-1311. 4. Thomas DM, et al. Brain Res, 2005, 1050(1-2), 190-198. 5. Brown TE, et al. Learn Mem, 2008, 15(12), 857-865. 6. Jiang L, et al. Decrease of growth and differentiation factor 10 contributes to neuropathic pain through N-methyl-D-aspartate receptor activation. Neuroreport. 2017 May 24;28(8):444-450.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

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

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

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。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 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 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

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 77086-22-7 Membrane transporter/Ion channel Neuroscience NMDAR iGluR MK 801 Maleate inhibit MK801 Maleate (+)-Mk-801 Hydrogen Maleate anticonvulsant MK 801 地卓亚平马来酸盐 neurotransmitter noncompetitive Dizocilpine hydrogen maleate ambulation MK801 voltage MK-801 hyperlocomotion MK-801 Maleate Ionotropic glutamate receptors 地佐环平马来酸盐 Dizocilpine hydrogen Maleate Inhibitor Mk-801 Hydrogen Maleate Dizocilpine (+)-MK 801 maleate (+)-MK 801 (Maleate) inhibitor

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Dizocilpine Maleate

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords