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Phenytoin Sodium is a potent Voltage-gated Na+ channels (VGSCs) blocker. The blocking of sodium channels by phenytoin is of slow onset. The time course of fast sodium currents is therefore not altered in the presence of the drug and action potentials evoked by synaptic depolarizations of ordinary duration are not blocked. Thus phenytoin is able to selectively inhibit pathological hyperexcitability in epilepsy without unduly impairing ongoing activity. Phenytoin also blocks persistent sodium current and this may be of particular importance in seizure control. Phenytoin has antiepileptic activity and reduces breast tumour growth and metastasis in mice.
| Molecular Weight | 274.25 |
| Formula | C15H11N2NaO2 |
| CAS Number | 630-93-3 |
| Solubility (25°C) | DMSO 42 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[1] Erenberk U, et al. Drug Chem Toxicol. Melatonin attenuates phenytoin sodium-induced DNA damage.
| Related Sodium Channel Products |
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| 5-(N,N-Hexamethylene)-amiloride
5-(N,N-Hexamethylene)-amiloride (Hexamethylene amiloride) is a potent Na+/H+ exchanger inhibitor, which decreases the intracellular pH (pHi) and induces apoptosis in leukemic cells. 5-(N,N-Hexamethylene)-amiloride (Hexamethylene amiloride) is also an inhibitor of the HIV-1 Vpu virus ion channel and inhibits mouse hepatitis virus (MHV) replication and human coronavirus 229E (HCoV229E) replication in cultured L929 cells with EC50s of 3.91 μM and 1.34 μM, respectively. |
| HwTx-IV
Huwentoxin-IV (HwTx-IV) is a 35-residue neurotoxin peptide with potential application as a novel analgesic. Huwentoxin-IV, a component of tarantula venom, potently blocks sodium channels and is an attractive scaffold for engineering a Nav1.7-selective molecule. |
| ST-2560
ST-2560 is a selective inhibitor of the NaV1.7 sodium channel with IC50 value of 39 nM in primates with ≥1000-fold selectivity over other isoforms of the human NaV1.x family. |
| A-317567
A-317567 is a potent acid-sensing ion channel 3 (ASIC-3) inhibitor with an IC50 of 1.025 μM. |
| XPC-6444
XPC-6444 is a highly potent, isoform-selective, and CNS-penetrant NaV1.6 inhibitor (IC50=41 nM for hNaV1.6). |
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