Dizocilpine maleate (Synonyms: (+)-MK 801 顺丁烯二酸盐; (+)-MK 801 Maleate)

目录号: HY-15084 纯度: 99.99%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Dizocilpine maleate (MK-801 maleate) 是一种有效，选择性，非竞争性的 NMDA 受体拮抗剂，K_d 值为 37.2 nM。

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Dizocilpine maleate Chemical Structure

CAS No. : 77086-22-7

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥512	In-stock
5 mg	￥290	In-stock
10 mg	￥465	In-stock
50 mg	￥1700	In-stock
100 mg		询价
200 mg		询价

or 大包装询价

* Please select Quantity before adding items.

Customer Review

Other Forms of Dizocilpine maleate:

(-)-Dizocilpine maleate In-stock
Dizocilpine In-stock

MCE 顾客使用本产品发表的 27 篇科研文献

: Dizocilpine maleate purchased from MCE. Usage Cited in: Cell Biosci. 2023 Mar 16;13(1):57. [Abstract]; Dizocilpine (MK-801; 1 mg/kg; i.v.; single) suppresses RIPC-induced SIRT3 upregulation in mice.

: Dizocilpine maleate purchased from MCE. Usage Cited in: J Cell Mol Med. 2020 Aug;24(16):9287-9299. [Abstract]; Neurons are pre-treated with 10 μM Dizocilpine (MK801), followed by TNF-α treatment (40 ng/mL, 2 h). MK801 could attenuate TNF-α- induced intracellular calcium accumulation, phosphorylation of CAMK II and calpain-2, calpain activation and cathepsin B release as well as TrkB truncation.

: Dizocilpine maleate purchased from MCE. Usage Cited in: Neuroreport. 2017 May 24;28(8):444-450. [Abstract]; Western blot analysis confirms that MK-801 inhibits the decrease in GDF10 in SNL rats. The relative expression level of GDF10 in the SNL-vehicle group is significantly decreased, but remains unchanged in the SNL-MK-801 group versus sham.

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AMPA Receptor NMDA Receptor Kainate Receptor

生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

Dizocilpine maleate (MK-801 maleate) is a potent, selective and non-competitive NMDA receptor antagonist with K_d of 37.2 nM in rat brain membranes.

IC₅₀ & Target

NMDA Receptor

体外研究
(In Vitro)

[³H]Dizocilpine maleate binds with NMDA receptor with a K_d of 37.2±2.7 nM in rat cerebral cortical membranes^[1].
Dizocilpine maleate causes a progressive, long-lasting blockade of current induced by N-Me-D-Asp^[3].
Dizocilpine maleate progressively suppresses of current induced by NMDA. Mg²⁺ (10 mM) prevents Dizocilpine from blocking the N-Me-D-Asp-induced current, even when Dizocilpine (MK-801) is applied for a long time in the presence of NMDA. Dizocilpine blocks NMDA-activated single-channel activity in outside-out patches^[3].
Dizocilpine maleate (< 500 μM) inhibits activation of microglia induced by LPS with increased Cox-2 protein expression in BV-2 cells. Dizocilpine (MK-801; <500 μM) reduces microglial TNF-α output with an EC₅₀ of 400 μM in BV-2 cells^[4].

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

体内研究
(In Vivo)

Dizocilpine maleate 可用于诱导精神分裂症模型。Dizocilpine maleate 在 SD 大鼠中，腹腔注射剂量为 0.2 mg/kg 时，半衰期为 52.31 分钟，曲线下面积 (AUC) 为 3185.48 nM·min，清除率为 34 mL/min/kg^[2]。

诱导精神分裂模型

致病原理

Dizocilpine maleate 诱导精神分裂的具体机制尚不清楚。一种假设是 Dizocilpine maleate 通过抑制 NMDA 致使谷氨酸能系统失调，从而诱导精神分裂。

具体造模方法：

大鼠：Sprague-Dawley • 雄性 • adult • 250-300 g
给药方式：0.4 mg/kg • 腹腔注射. • 单剂量

Note

造模成功指标

行为：自发活动增加并伴有明显的焦虑样行为，具体表现为较远距离运动活动增加 (多动)，在中心区停留时间减少 (回避中心区)。
前脉冲抑制 (PPI)：PPI 显著降低。
迷宫测试：在高架十字迷宫测试中表现为避免进入开阔臂，在 Y 迷宫测试中表现为减少进入新臂

相关产品： Phencyclidine

拮抗产品： Clozapine (HY-14539); Haloperidol (HY-14538)

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

分子量

337.37

Formula

C₂₀H₁₉NO₄

CAS 号

77086-22-7

性状

固体

颜色

White to off-white

中文名称

(+)-MK 801 顺丁烯二酸盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

溶解性数据

细胞实验：

DMSO 中的溶解度 : 133.33 mg/mL (395.20 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

Ethanol 中的溶解度 : 25 mg/mL (74.10 mM; 超声助溶)

H₂O 中的溶解度 : 7.69 mg/mL (22.79 mM; 超声助溶)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.9641 mL	14.8205 mL	29.6410 mL
5 mM	0.5928 mL	2.9641 mL	5.9282 mL
10 mM	0.2964 mL	1.4821 mL	2.9641 mL

查看完整储备液配制表

* 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, 2 years; -20°C, 1 year (sealed storage, away from moisture)。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% EtOH 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.41 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 EtOH 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% EtOH 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.41 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 EtOH 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
20% SBE-β-CD in Saline 的配制（4°C，储存一周）：2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.19 mg/mL (6.49 mM); 澄清溶液

此方案可获得 ≥ 2.19 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 21.9 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案四

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (6.17 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
20% SBE-β-CD in Saline 的配制（4°C，储存一周）：2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案五

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (6.17 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。

方案一

请依序添加每种溶剂： Saline
Solubility: 3.45 mg/mL (10.23 mM); 澄清溶液; 超声助溶

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

*In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.99%

选择批次：

Data Sheet (666 KB) SDS (393 KB)

COA (299 KB) HNMR (142 KB) RP-HPLC (243 KB) LCMS (87 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Wong EH, et al. The anticonvulsant MK-801 is a potent N-Me-D-Asp antagonist. Proc Natl Acad Sci U S A. 1986 Sep;83(18):7104-8. [Content Brief]

[2]. Vardhan Reddy KH, et al. Convergent Strategy to Dizocilpine MK-801 and Derivatives. J Org Chem. 2018 Apr 6;83(7):4264-4269. [Content Brief]

[3]. Huettner JE, et al. Block of N-Me-D-Asp-activated current by the anticonvulsant MK-801: selective binding to open channels. Proc Natl Acad Sci U S A. 1988 Feb;85(4):1307-11. [Content Brief]

[4]. Thomas DM, et al. MK-801 and dextromethorphan block microglial activation and protect against neurotoxicity. Brain Res. 2005 Jul 19;1050(1-2):190-8. [Content Brief]

[5]. Brown TE, et al. The NMDA antagonist MK-801 disrupts reconsolidation of a cocaine-associated memory for conditioned place preference but not for self-administration in rats. Learn Mem. 2008 Dec 2;15(12):857-65. [Content Brief]

[6]. Iijima Y, et al. Modification by MK-801 (dizocilpine), a noncompetitive NMDA receptor antagonist sensitization: evaluation by ambulation in mice. Nihon Shinkei Seishin Yakurigaku Zasshi. 1996 Feb;16(1):11-8. [Content Brief]

[7]. Jiang L, et al. Decrease of growth and differentiation factor 10 contributes to neuropathic pain through N-Me-D-Asp receptor activation. Neuroreport. 2017 May 24;28(8):444-450. [Content Brief]

Animal Administration ^[5]	Animals are given saline or Dizocilpine ((+)-MK 801) followed by cocaine 30 min later in the home cage instead of in the CPP apparatus for the two days of “reactivation.” This is done to determine whether reactivation of the memory for the cocaine-associated context by cocaine in the CPP context is necessary for the ability of Dizocilpine ((+)-MK 801) to disrupt reconsolidation. Animals undergo preconditioning, conditioning, testing, and extinction but animals are injected with saline or Dizocilpine ((+)-MK 801) (0.20 mg/kg, i.p.) 30 min prior to a cocaine injection (10 mg/kg, i.p.) in the home cage. Animals remain in the home cages, and the next day, the procedure from the first day of reactivation is repeated. The following day, animals are tested for cocaine-primed reinstatement in their CPP box without any prior microinjection of saline or Dizocilpine ((+)-MK 801). MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Wong EH, et al. The anticonvulsant MK-801 is a potent N-Me-D-Asp antagonist. Proc Natl Acad Sci U S A. 1986 Sep;83(18):7104-8. [Content Brief] [2]. Vardhan Reddy KH, et al. Convergent Strategy to Dizocilpine MK-801 and Derivatives. J Org Chem. 2018 Apr 6;83(7):4264-4269. [Content Brief] [3]. Huettner JE, et al. Block of N-Me-D-Asp-activated current by the anticonvulsant MK-801: selective binding to open channels. Proc Natl Acad Sci U S A. 1988 Feb;85(4):1307-11. [Content Brief] [4]. Thomas DM, et al. MK-801 and dextromethorphan block microglial activation and protect against neurotoxicity. Brain Res. 2005 Jul 19;1050(1-2):190-8. [Content Brief] [5]. Brown TE, et al. The NMDA antagonist MK-801 disrupts reconsolidation of a cocaine-associated memory for conditioned place preference but not for self-administration in rats. Learn Mem. 2008 Dec 2;15(12):857-65. [Content Brief] [6]. Iijima Y, et al. Modification by MK-801 (dizocilpine), a noncompetitive NMDA receptor antagonist sensitization: evaluation by ambulation in mice. Nihon Shinkei Seishin Yakurigaku Zasshi. 1996 Feb;16(1):11-8. [Content Brief] [7]. Jiang L, et al. Decrease of growth and differentiation factor 10 contributes to neuropathic pain through N-Me-D-Asp receptor activation. Neuroreport. 2017 May 24;28(8):444-450. [Content Brief]

Animal Administration
^[5]

Animals are given saline or Dizocilpine ((+)-MK 801) followed by cocaine 30 min later in the home cage instead of in the CPP apparatus for the two days of “reactivation.” This is done to determine whether reactivation of the memory for the cocaine-associated context by cocaine in the CPP context is necessary for the ability of Dizocilpine ((+)-MK 801) to disrupt reconsolidation. Animals undergo preconditioning, conditioning, testing, and extinction but animals are injected with saline or Dizocilpine ((+)-MK 801) (0.20 mg/kg, i.p.) 30 min prior to a cocaine injection (10 mg/kg, i.p.) in the home cage. Animals remain in the home cages, and the next day, the procedure from the first day of reactivation is repeated. The following day, animals are tested for cocaine-primed reinstatement in their CPP box without any prior microinjection of saline or Dizocilpine ((+)-MK 801).

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

参考文献

[1]. Wong EH, et al. The anticonvulsant MK-801 is a potent N-Me-D-Asp antagonist. Proc Natl Acad Sci U S A. 1986 Sep;83(18):7104-8. [Content Brief]

[2]. Vardhan Reddy KH, et al. Convergent Strategy to Dizocilpine MK-801 and Derivatives. J Org Chem. 2018 Apr 6;83(7):4264-4269. [Content Brief]

[3]. Huettner JE, et al. Block of N-Me-D-Asp-activated current by the anticonvulsant MK-801: selective binding to open channels. Proc Natl Acad Sci U S A. 1988 Feb;85(4):1307-11. [Content Brief]

[4]. Thomas DM, et al. MK-801 and dextromethorphan block microglial activation and protect against neurotoxicity. Brain Res. 2005 Jul 19;1050(1-2):190-8. [Content Brief]

[5]. Brown TE, et al. The NMDA antagonist MK-801 disrupts reconsolidation of a cocaine-associated memory for conditioned place preference but not for self-administration in rats. Learn Mem. 2008 Dec 2;15(12):857-65. [Content Brief]

[6]. Iijima Y, et al. Modification by MK-801 (dizocilpine), a noncompetitive NMDA receptor antagonist sensitization: evaluation by ambulation in mice. Nihon Shinkei Seishin Yakurigaku Zasshi. 1996 Feb;16(1):11-8. [Content Brief]

[7]. Jiang L, et al. Decrease of growth and differentiation factor 10 contributes to neuropathic pain through N-Me-D-Asp receptor activation. Neuroreport. 2017 May 24;28(8):444-450. [Content Brief]

Dizocilpine maleate 相关分类

Neurological Disease

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

H₂O / Ethanol / DMSO	1 mM	2.9641 mL	14.8205 mL	29.6410 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
	15 mM	0.1976 mL	0.9880 mL	1.9761 mL	4.9402 mL
	20 mM	0.1482 mL	0.7410 mL	1.4821 mL	3.7051 mL
Ethanol / DMSO	25 mM	0.1186 mL	0.5928 mL	1.1856 mL	2.9641 mL
	30 mM	0.0988 mL	0.4940 mL	0.9880 mL	2.4701 mL
	40 mM	0.0741 mL	0.3705 mL	0.7410 mL	1.8526 mL
	50 mM	0.0593 mL	0.2964 mL	0.5928 mL	1.4821 mL
	60 mM	0.0494 mL	0.2470 mL	0.4940 mL	1.2350 mL
DMSO	80 mM	0.0371 mL	0.1853 mL	0.3705 mL	0.9263 mL
DMSO	100 mM	0.0296 mL	0.1482 mL	0.2964 mL	0.7410 mL

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

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Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Dizocilpine77086-22-7(+)-MK 801(+)-MK 801 顺丁烯二酸盐iGluRIonotropic glutamate receptorsnoncompetitiveambulationhyperlocomotionanticonvulsantneurotransmittervoltageInhibitorinhibitorinhibit

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Dizocilpine maleate (Synonyms: (+)-MK 801 顺丁烯二酸盐; (+)-MK 801 Maleate)

Customer Review

Other Forms of Dizocilpine maleate:

MCE 顾客使用本产品发表的 27 篇科研文献

Dizocilpine maleate 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 iGluR 亚型特异性产品:

生物活性

实验参考方法

纯度 & 产品资料

参考文献

摩尔计算器

稀释计算器

Dizocilpine maleate 相关分类

完整储备液配制表

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Dizocilpine maleate (Synonyms: (+)-MK 801 顺丁烯二酸盐; (+)-MK 801 Maleate)

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