Oxidopamine (hydrobromide) [636-00-0]

Referência HY-B1081A-200mg

Tamanho : 200mg

Marca : MedChemExpress

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Description

Oxidopamine (6-OHDA) hydrobromide is an antagonist of the neurotransmitter dopamine. Oxidopamine hydrobromide is a widely used neurotoxin and selectively destroys dopaminergic neurons. Oxidopamine hydrobromide promotes COX-2 activation, leading to PGE2 synthesis and pro-inflammatory cytokine IL-1β secretion. Oxidopamine hydrobromide can be used for the research of Parkinson’s disease (PD), attention-deficit hyperactivity disorder (ADHD), and Lesch-Nyhan syndrome[1][2][3][4].

IC50 & Target

COX-2

 

IL-1β

 

Caspase-3

 

Caspase-8

 

Caspase-9

 

In Vitro

Oxidopamine hydrobromide (0-500 μM, 24 h) decreases the viability of both Neuro-2a cells and SH-SY5Y cells in a concentration-dependent manner[1].
Oxidopamine hydrobromide (75-150 μM, 0-24 h) induces COX-2 expression and nuclear translocation[1].
Oxidopamine hydrobromide (75-150 μM, 0-24 h) causes PGE2 biosynthesis and pro-inflammatory cytokine IL-1β production[1].
Oxidopamine hydrobromide (0-150 μM, 12 h) induces apoptosis and mitochondrial membrane depolarization of pheochromocytoma PC12 cells[3].
Oxidopamine hydrobromide (75 μM, 0-12 h) induces p38 phosphorylation[3].

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

Cell Viability Assay[1]

Cell Line: Neuro-2a cells and SH-SY5Y cells
Concentration: 0-500 µM
Incubation Time: 24 or 48 h
Result: Induced neurotoxicity, caused cytotoxicity in both Neuro-2a cells and SH-SY5Y cells in a concentration dependent manner. EC50=111 µM for 24 h incubation and 109 µM for 48 h incubation in the Neuro-2a cells; EC50=118 µM for 24 h incubation and 107 µM for 48 h incubation in the SH-SY5Y cells.

RT-PCR[1]

Cell Line: Neuro-2a cells and SH-SY5Y cells
Concentration: 75 or 150 µM
Incubation Time: 0, 6 or 24 h
Result: Quickly and robustly induced COX-2 in a time-dependent manner. Induced COX-2 activation characterized by expression induction and nuclear translocation. Substantially increased PGE2 in the culture medium by nearly 5-fold in Neuro-2a cells (at 75 µM) and 3-fold in SH-SY5Y cells (at 150 µM). Significantly upregulated the pro-inflammatory cytokine interleukin-1β (IL-1β) within Neuro-2a cells and SH-SY5Y cells.

Apoptosis Analysis[3]

Cell Line: PC12 cells
Concentration: 0, 25, 50, 75, and 150 μM
Incubation Time: 0, 2, 4, 6, 12, and 20 h
Result: Induced apoptosis of PC12 cells. Increased the activities of caspase-3, -8 and -9 in PC12 cells in a time- and concentration-dependent manner. Increased these caspase activities at 2-4 h and reached a maximum at 12 h. Decreased cells with high mitochondrial membrane potential (JC-1 aggregate) in a time- and concentration-dependent manner.

Western Blot Analysis[3]

Cell Line: PC12 cells
Concentration: 75 μM
Incubation Time: 0, 3, 5, 6, 8, 10, and 12 h
Result: Increased the level of p-p38 in a time-dependent manner.
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.

Oxidopamine (6-OHDA) hydrobromide can induce Parkinson's disease models[5][6].

Induction of Parkinson's disease model[5][6][7]
Background
The chemical structure of Oxidopamine (6-OHDA) hydrobromide is similar to dopamine (DA), enabling it to compete with DA for uptake sites and be subsequently taken into cells. Once inside the cells, oxidopamine hydrochloride can be oxidized and decomposed, generating reactive oxygen species, which further produce oxygen free radicals through MAO (monoamine oxidase) or directly cause mitochondrial dysfunction, leading to the death of dopaminergic neurons.
Specific Modeling Methods
Rat: Sprague-Dawley (SD) • Male • 200-250 g;
Administration: 5μg/2μL/site • stereotaxically injected in the fight striatum • single dose.
Solvent: dissolved in 0.1%-0.2% Ascorbic acid in PBS or 0.01%-0.02% Ascorbic acid in saline.
Note
Oxidopamine hydrobromide is commonly dissolved in 0.02% Ascorbic acid in saline or 0.02% Ascorbic acid in PBS in the literature. L‑Ascorbic acid (HY‑B0166) (ascorbic acid) has been reported to possess antioxidant properties, which can prevent the degradation of Oxidopamine.
(1) Lesions were made by the unilateral injection of Oxidopamine hydrobromide (5 μg in 2 μl/site) into the right striatum at the two coordinates:
① AP, 0.7; L, 3.0; DV, 5.5 and 4.5 mm from Bregma.
② AP, 0.2; L, 2.6; DV, 5.5 and 4.5 mm from Bregma.
The two coordinates were injected Oxidopamine hydrobromide 10 μg in 4 μl/2 sites.
(2) Oxidopamine hydrobromide was prepared freshly in dark to avoid autooxidation, and was administered using a 5 μl microinjector at a rate of 0.5 μl/min. The syringe was left in place for 5 min before slowly retracting it to allow for toxin diffusion and prevent the toxin reflux.
(3) On the 56th day after the injury, the animals were decapitated under deep halothane anesthesia. Their brains were quickly removed from the skull, rinsed with chilled saline, and tissue samples containing the caudate-putamen head were dissected from both the lesioned and unlesioned striata on ice.
(4) The animals were housed in an environment with a 12-hour light/dark cycle, with the temperature maintained at 22-23°C. They were allowed free access to food and tap water.
Modeling Indicators
Behavioral monitoring: Rats exhibit rotation with a rotation count greater than 210 r/30 min. Molecular changes: Elevated levels of COX-2, TNF-α mRNA, and COX-2 protein. Histopathological changes: Chromatin condensation into clumps around the nucleus, along with evident mitochondrial swelling and vacuolation. Induced nigrostriatal nerve terminal lesions. Decreased striatal dopamine levels and reduced number of tyrosine hydroxylase immunoreactive cells in the ipsilateral substantia nigra, accompanied by long-term significant atrophy of remaining dopaminergic neurons.
Opposite Product(s): Resveratrol (HY-16561)

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

Masse moléculaire

250.09

Formule

C8H12BrNO3

CAS No.
Appearance

Solid

Color

Light brown to gray

SMILES

OC1=CC(CCN)=C(O)C=C1O.10Br

Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

4°C, stored under nitrogen, away from moisture

*The compound is unstable in solutions, freshly prepared is recommended.

Solvant et solubilité
In Vitro: 

DMSO : 50 mg/mL (199.93 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 20 mg/mL (79.97 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.9986 mL 19.9928 mL 39.9856 mL
5 mM 0.7997 mL 3.9986 mL 7.9971 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

* 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:  0.02% Ascorbic acid in PBS

    Solubility: 50 mg/mL (199.93 mM); Clear solution; Need ultrasonic

  • Protocol 2

    Add each solvent one by one:  0.02% Ascorbic acid in Saline water

    Solubility: 50 mg/mL (199.93 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Pureté et documentation
Références

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