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Carbamazepine is a sodium channel inhibitor with an IC50 of 131 μM when treated with synaptosomes in rat brain. Carbamazepine blocks voltage gated Na+, Ca2+, and K+ channels, and is also a HDAC inhibitor (IC50=2 μM). Voltage-gated sodium channels are the molecular pores that allow brain cells (neurons) to generate action potentials, the electrical events that allow neurons to communicate over long distances. After the sodium channels open to start the action potential, they inactivate, essentially closing the channel. Carbamazepine stabilizes the inactivated state of sodium channels, meaning that fewer of these channels are available to subsequently open, making brain cells less excitable.
| Cell Experiment | |
|---|---|
| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
|---|---|
| Animal models | Male Wistar rats |
| Formulation | Dissolved in saline/DMSO (50/50 vol/vol) |
| Dosages | ~100 mg/kg |
| Administration | Injected intraperitoneally (i.p.) |
| Molecular Weight | 236.27 |
| Formula | C15H12N2O |
| CAS Number | 298-46-4 |
| Form | Solid |
| Solubility (25°C) | DMSO ≥ 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[7] R H Levy, et al. Clinical pharmacokinetics of carbamazepine
| Related Sodium Channel Products |
|---|
| 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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