pt en es

Reagentes e instrumentos para imunologia, biologia celular e biologia molecular.

Dizocilpine (maleate) [77086-22-7]

Imprimir

Referência HY-15084-10mg

Tamanho : 10mg

Contactar o distribuidor local :

Telefone : +1 850 650 7790

Marca : MedChemExpress

Solicitar mais informações

Contactar o distribuidor local :

Telefone : +1 850 650 7790

Description

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

Cellular Effect

Cell Line	Type	Value	Description	References
SH-SY5Y	IC₅₀	7.91 nM Compound: MK-801	Neuroprotective activity in human SH-SY5Y cells assessed as protection against NMDA-induced cell death after 6 hrs by MTS assay Neuroprotective activity in human SH-SY5Y cells assessed as protection against NMDA-induced cell death after 6 hrs by MTS assay	[PMID: 23033965]

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].

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

In Vivo

Note:
Please do not refer to only one article to determine the experimental conditions. It is recommended to determine the optimal experimental conditions (animal strain, age, dosage, frequency and cycle, detection time and indicators, etc.) through preliminary experiments before the formal experiment.

Dizocilpine maleate can be used to induce schizophrenia models. In SD rats, when administered intraperitoneally at a dose of 0.2 mg/kg, Dizocilpine maleate has a half-life of 52.31 minutes, an area under the curve (AUC) of 3185.48 nM·min, and a clearance rate of 34 mL/min/kg^[2].

Induction of Schizophrenia

Background

The specific mechanism of schizophrenia induction is unclear. One hypothesis is that, Dizocilpine maleateleads to dysregulation of glutamatergic system through NMDA inhibition^[2].

Specific Modeling Methods

Rat: Sprague-Dawley • male • adult with weight of 250-300 g
Administration: 0.4 mg/kg • i.p. • single dose.

Note

Dizocilpine maleate is dissolved in 0.9% sterile saline.

Modeling Indicators

Behavior: Increased spontaneous activity with obvious anxiety-like behavior, increased motor activity in longer diatance (hyperactivity), reduced time staying in central area (avoidance of central area).
Prepulse Inhibition (PPI): Decreased PPI significantly.
maze test:Avoided open arm entries in elevated plus maze test and reduced number of novel arm entries in Y maze test.

Correlated Product(s): Phencyclidine

Opposite Product(s): Clozapine (HY-14539); Haloperidol (HY-14538)

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

Masse moléculaire

337.37

Formule

C₂₀H₁₉NO₄

CAS No.

77086-22-7

Appearance

Solid

Color

White to off-white

SMILES

C[C@]12C3=CC=CC=C3C[C@@H](N2)C4=CC=CC=C14.O=C(O)/C=C\C(O)=O

Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

4°C, sealed storage, away from moisture

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

Solvant et solubilité

In Vitro:

DMSO : 133.33 mg/mL (395.20 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : 25 mg/mL (74.10 mM; Need ultrasonic)

H₂O : 7.69 mg/mL (22.79 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% EtOH 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.41 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% EtOH 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.41 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.19 mg/mL (6.49 mM); Clear solution

This protocol yields a clear solution of ≥ 2.19 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.9 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 4

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (6.17 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 5

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (6.17 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: Saline
Solubility: 3.45 mg/mL (10.23 mM); Clear solution; Need ultrasonic

Pureté et documentation

Purity: 99.99%

Fiche technique (293 KB) SDS (393 KB)

COA (261 KB) HNMR (142 KB) RP-HPLC (243 KB) LCMS (86 KB)

Instruction de manipulation (2659 KB)

Références

[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]. Wegener N, et al. Evaluation of brain pharmacokinetics of (+)MK-801 in relation to behaviour. Neurosci Lett. 2011 Sep 26;503(1):68-72. [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]

Você também pode estar interessado nos seguintes produtos:

Referência

Descrição

Cond.

Price Bef. VAT

0413-SC

Poly-L-Lysine

10mg/ml

Dizocilpine (maleate) [77086-22-7]

Referência HY-15084-10mg

Contactar o distribuidor local :

Marca : MedChemExpress

Contactar o distribuidor local :

Dizocilpine maleate Related Antibodies

Você também pode estar interessado nos seguintes produtos: