Primidone [125-33-7]

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Katalog-Nummer T0024-100mg

Size : 100mg

Marke : 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.
Primidone
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
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.
SynonymsPrimaclone, NCI-C56360, Mysoline
Chemical Properties
Molecular Weight218.25
FormulaC12H14N2O2
Cas No.125-33-7
SmilesCCC1(C(=O)NCNC1=O)C1=CC=CC=C1
Relative Density.1.138g/cm3
Storage & Solubility Information
StoragePowder: -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
1mg5mg10mg50mg
1 mM4.5819 mL22.9095 mL45.8190 mL229.0951 mL
5 mM0.9164 mL4.5819 mL9.1638 mL45.8190 mL
10 mM0.4582 mL2.2910 mL4.5819 mL22.9095 mL
20 mM0.2291 mL1.1455 mL2.2910 mL11.4548 mL
50 mM0.0916 mL0.4582 mL0.9164 mL4.5819 mL
100 mM0.0458 mL0.2291 mL0.4582 mL2.2910 mL
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.

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