| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| Other Sizes |
| Targets |
Free radicals and MMP-9 (matrix metalloproteinase-9). Edaravone acts as a free radical scavenger, reducing oxidative stress and inhibiting MMP-9-related brain hemorrhage.
|
|---|---|
| ln Vitro |
Edaravone D5 is a deuterium-labeled analog of edaravone. The parent compound is a strong free radical scavenger that effectively prevents MMP-9-related brain hemorrhage in rats treated with tissue plasminogen activator. Edaravone has neuroprotective effects and is used clinically for acute ischemic stroke and ALS. It scavenges hydroxyl radicals and inhibits lipid peroxidation.
|
| ln Vivo |
Edaravone D5 is primarily used as an analytical reference standard. The parent compound edaravone has been evaluated in clinical trials for acute ischemic stroke and ALS. It is administered intravenously and has a short half-life. Edaravone is well tolerated and shows neuroprotective effects in animal models of cerebral ischemia.
|
| Enzyme Assay |
The free radical scavenging assay measures the ability of edaravone to scavenge hydroxyl radicals or other reactive oxygen species. The assay uses a fluorescent probe or colorimetric reagent to detect radical levels in the presence or absence of test compound. IC50 values are calculated from dose-response curves.
|
| Cell Assay |
Cell-based assays for neuroprotective activity use primary neurons or neuronal cell lines exposed to oxidative stress (e.g., H2O2 or glutamate). Cells are treated with serially diluted edaravone D5, and cell viability is assessed by MTT or ATP-based assays. Intracellular reactive oxygen species levels are measured by fluorescent probes.
|
| Animal Protocol |
In vivo studies with Edaravone D5 focus on pharmacokinetic characterization. Rats or mice are administered edaravone, and plasma concentrations are measured by LC-MS/MS using the deuterated internal standard. Parameters such as Cmax, Tmax, AUC, t1/2, and clearance are determined. Neuroprotective efficacy is assessed in animal models of cerebral ischemia by measuring infarct volume and neurological deficit scores.
|
| References |
|
| Molecular Formula |
C10H10N2O
|
|---|---|
| Molecular Weight |
179.2300
|
| Exact Mass |
179.111
|
| CAS # |
1228765-67-0
|
| Related CAS # |
Edaravone;89-25-8
|
| PubChem CID |
46215970
|
| Appearance |
Off-white to light yellow solid powder
|
| LogP |
1.299
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
1
|
| Heavy Atom Count |
13
|
| Complexity |
241
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
[2H]C1=C(C(=C(C(=C1[2H])[2H])N2C(=O)CC(=N2)C)[2H])[2H]
|
| InChi Key |
QELUYTUMUWHWMC-VIQYUKPQSA-N
|
| InChi Code |
InChI=1S/C10H10N2O/c1-8-7-10(13)12(11-8)9-5-3-2-4-6-9/h2-6H,7H2,1H3/i2D,3D,4D,5D,6D
|
| Chemical Name |
5-methyl-2-(2,3,4,5,6-pentadeuteriophenyl)-4H-pyrazol-3-one
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 5.5794 mL | 27.8971 mL | 55.7942 mL | |
| 5 mM | 1.1159 mL | 5.5794 mL | 11.1588 mL | |
| 10 mM | 0.5579 mL | 2.7897 mL | 5.5794 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
