Primidone [125-33-7]
Référence T0024-100mg
Conditionnement : 100mg
Marque : TargetMol
Primidone
(Synonyms: Primaclone, NCI-C56360, Mysoline) Copy Product Info
Primidone (NCI-C56360) is a potent anticonvulsant agent. It is a neuronal voltage-gated sodium channel blocker and has value in the study of epilepsy, essential tremor, and psychiatric disorders.
Cas No. 125-33-7
For research use only—not for human use. No sales to individuals. Use as intended only.
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Purity:99.91%
Appearance:Solid
Color:White
COA HNMR LCMS
Product Introduction
Primidone AI Summary
Primidone exhibits a diverse range of bioactivities, including significant inhibitory effects against various enzymes and receptors, as well as notable anticonvulsant, sedative, and antiviral properties. In enzymatic assays, it demonstrates less than 5.0% inhibition of beta-lactamase and chymotrypsin at concentrations of 100 uM and 250 uM, respectively, but shows 13.0% inhibition of malate dehydrogenase (MDH) at 400 uM. It also exhibits broad-spectrum inhibition against targets such as Tyrosyl-DNA Phosphodiesterase, DNA Polymerase Beta, Histone Lysine Methyltransferase G9a, and Cytochrome p450-cyp1a2, among others. Additionally, Primidone shows anticonvulsant and sedative effects with a median effective dose (ED50) of 58.6 mg/kg in the subcutaneous metrazole test. It acts as an agonist at the Thyroid Stimulating Hormone Receptor and androgen receptor signaling pathways. Furthermore, the compound demonstrates high oral bioavailability in humans, with an F value of 92.0% and a logD value of 0.91, indicating favorable partitioning properties. In antiviral assays, Primidone inhibits SARS-CoV-2-induced cytotoxicity in Caco-2 and Vero E6 cells, showing specific inhibition rates and hit scores that suggest moderate activity against the virus. It also displays inhibitory activity against the SARS-CoV-2 3CL-Pro protease. In terms of liver toxicity, Primidone shows no significant adverse effects on hepatic functions, with a severity class index for drug-induced liver injury of 0.0. It also inhibits sodium fluorescein uptake in OATP1B3 and OATP1B1 CHO cells, suggesting potential implications in drug transport interactions. Lastly, the compound has been found to have antifungal and antibacterial activity against various pathogens, including Candida albicans, Cryptococcus neoformans, and multiple bacterial strains such as Acinetobacter baumannii and Staphylococcus aureus MRSA. Overall, Primidone presents a versatile pharmacological profile with potential therapeutic applications across several domains..
Note: Summary generated by AI. Data source: ChEMBL 
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | Primidone (NCI-C56360) is a potent anticonvulsant agent. It is a neuronal voltage-gated sodium channel blocker and has value in the study of epilepsy, essential tremor, and psychiatric disorders. |
| Synonyms | Primaclone, NCI-C56360, Mysoline |
| Molecular Weight | 218.25 |
| Formula | C12H14N2O2 |
| Cas No. | 125-33-7 |
| Smiles | CCC1(C(=O)NCNC1=O)C1=CC=CC=C1 |
| Relative Density. | 1.138g/cm3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 70 mg/mL (320.73 mM), Sonication is recommended.  | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (9.16 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | ||||||||||||||||||||||||||||||||||||