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| 5g |
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| 25g |
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Purity: ≥98%
Edaravone (formerly known as Radicut; MCI-186; NCI-C03952; NSC 12; Norantipyrine; Norphenazone; trade name: Radicava) is a novel and potent free radical scavenger that has been used clinically to reduce the neuronal damage following ischemic stroke. In May 2017, Edaravone was approved by FDA to treat patients with amyotrophic lateral sclerosis (ALS). Edaravone inhibits MMP-9-related brain hemorrhage in rats treated with tissue plasminogen activator. It was approved by FDA in May 5th 2017 for the treatment of amyotrophic lateral sclerosis (ALS). Edaravone reduces apoptosis and necrosis caused by glutamate. Pretreatment of edaravone (500 μM) reverses these changes to approximately normal levels.
| Targets |
MMP-9-related brain hemorrhage
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| ln Vitro |
Edaravone has effects on glutamate toxicity that are both therapeutic and preventative. Edaravone pretreatment decreased glutamate's toxicity to SGN. Edaravone lessens necrosis and apoptosis brought on by glutamate. These alterations were reverted to near-normal levels by pretreatment with 500 μM edaravone. Edaravone's protective action against glutamate-induced SGNs cell apoptosis is associated with the Bcl-2 protein family and the PI3K/Akt pathway [4].
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| ln Vivo |
In cerebral ischemia, edaravone reduces neuronal damage and prevents endothelium damage to have neuroprotective effects. The helpful NOS that can save an ischemic stroke is increased when eNOS is present, but nNOS and iNOS—the toxic NOS—are decreased when edaravone is present. Pretreatment with edaravone decreases hemorrhagic episodes and post-reperfusion cerebral edema brought on by thrombolytic therapy [1]. The infarct size was greatly reduced by edaravone; rats in the edaravone group had an average infarct size of 227.6 mm3, which was significantly smaller than rats in the control group (264.0 mm3). Additionally, the post-ischemic bleeding volume was decreased by edaravone therapy (53.4 mm3 in edaravone-treated rats against 53.4 mm3 in the control group). 176.4 millimeters). Furthermore, rats treated with edaravone had a decreased ratio of bleeding volume to infarct volume (23.5%) compared to rats not treated (63.2%) [2]. The corpus callosum, germinal matrix, and cerebral cortex of rats given Edaravone (20 mg/kg) showed decreased astrocyte activity (glial fibrillary acidic protein) and apoptotic cells (caspase-3) [3].
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| Enzyme Assay |
Detection of Apoptosis and Necrosis by Ho.33342 and Propidium Iodide (PI) Double Staining [4]
SGNs were incubated with glutamate with or without edaravone (500 μM). Control cells were without any treatment. Cells were washed twice by PBS, fixed with 95% alcohol for 10 min, and then stained by Ho.33342 (10 mg/mL) and PI (50 mg/mL) at 37°C for 30 min. Morphological changes were examined by fluorescence microscope under green light (515–560 nm) and ultraviolet (UV) light (340–380 nm), respectively. At least 500 cells were counted in 5 randomly selected fields per group. All treatments were repeated three times. Detection of GSH Content, SOD Activity, and MDA Level by Spectrophotometer[4] SGNs were incubated with 2 mM glutamate for 10 min with or without the pretreatment of 500 μM edaravone 2 h ahead. Control cells were without any treatment. Then cells were washed twice with ice-cold PBS, sonicated, and harvested for the following assays. Intracellular GSH content, SOD activity, and MDA level in all groups were measured by commercial assay kits according to the manufacturer's instructions. OD values at optimal wavelengths were measured using spectrophotometer and the relative levels comparing with control cells were calculated. All experiments were repeated three times. |
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| Cell Assay |
Drug Treatment [4]
SGNs (1.0 × 105/mL) subcultured in 96-well or 24-well plate were treated with 2 mM glutamate for 10 minutes. Then the medium was replaced by normal DMEM. Different concentrations of edaravone were added to the medium either 20 min before or 2 h, 6 h, and 12 h after glutamate treatment. All the doses and time points were determined by preliminary experiments (data not shown). Assessment of Cell Viability by MTT and Trypan Blue Staining[4] Cell viability was quantified by MTT assay and trypan blue staining. MTT (5 mg/mL, 20 μL) was added to each well and incubated for 4 h at 37°C after the drug treatments as described above. The medium was removed and the cell pellet was dissolved in DMSO. Then, the optical density (OD) values were measured at 570 nm using an ELISA reader. All experiments were repeated three times. Cell relative viability was calculated according to the following formula: Cell relative viability (%)=ODexperimentODcontrol×100%. ODblank was used as zero. In trypan blue staining, SGNs were stained with 0.4% trypan blue for 5 min after the drug treatments as described above. Pictures were taken by microscope and trypan blue positive and negative cells were counted afterwards. Cell survival rate was defined as the percentage of negative cells. |
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| Animal Protocol |
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| References |
[1]. Yoshida, H., et al. Neuroprotective effects of edaravone: a novel free radical scavenger in cerebrovascular injury. CNS Drug Rev, 2006. 12(1): p. 9-20.
[2]. Okamura, K., et al. Edaravone, a free radical scavenger, attenuates cerebral infarction and hemorrhagic infarction in rats with hyperglycemia. Neurol Res, 2013. [3]. Garcia CA, et al. Edaravone reduces astrogliosis and apoptosis in young rats with kaolin-induced hydrocephalus. Childs Nerv Syst. 2016 Dec 17. [Epub ahead of print] [4]. Bai X, et al. Protective Effect of Edaravone on Glutamate-Induced Neurotoxicity in Spiral Ganglion Neurons. Neural Plast. 2016;2016:4034218. Epub 2016 Nov 10 |
| Molecular Formula |
C10H10N2O
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| Molecular Weight |
174.2
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| Exact Mass |
174.0793
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| Elemental Analysis |
C, 68.95; H, 5.79; N, 16.08; O, 9.18
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| CAS # |
89-25-8
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| Related CAS # |
Edaravone-d5;1228765-67-0
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| Appearance |
Light yellow to yellow solid
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| LogP |
0.44
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| tPSA |
32.67
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| SMILES |
O=C1CC(C)=NN1C2=CC=CC=C2
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| InChi Key |
QELUYTUMUWHWMC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C10H10N2O/c1-8-7-10(13)12(11-8)9-5-3-2-4-6-9/h2-6H,7H2,1H3
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| Chemical Name |
5-methyl-2-phenyl-2,4-dihydro-3H-pyrazol-3-one
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| Synonyms |
MCI-186; NCI-C03952; MCI 186; NSC 12; MCI186; Radicut; trade name: Radicava; Methylphenylpyrazolone; Norantipyrine; Norphenazone; Phenylmethylpyrazolone; Arone
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (14.35 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (14.35 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (14.35 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 5.7405 mL | 28.7026 mL | 57.4053 mL | |
| 5 mM | 1.1481 mL | 5.7405 mL | 11.4811 mL | |
| 10 mM | 0.5741 mL | 2.8703 mL | 5.7405 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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