Retigabine (Ezogabine, D-23129) is an anticonvulsant for KCNQ2/3 currents with EC50 of 3.6 μM. Retigabine is a KCNQ/Kv7 potassium channel activator which functions by enhancing potassium currents via stabilizing the open conformation of the Kv7.2-7.3 channels. Studies indicate that the agonist binds in between two subunits of the channel which allows it to stabilize the channels open conformation. In addition, KCNQ3, a type of KCNQ channel, includes a hydrophobic pocket which contains a Leu338 region which is the binding site for retigabine. Furthermore, Retigabine has been shown to accelerate the activation of neuronal resting potentials while slowing deactivation of these currents. Secondly, Retigabine selectively activates the KCNQ2-5 isoforms, which results in an increased open channel probability. Studies also indicate that this compound can act as a GABA enhancer via amplifying the production of GABA in cortical neurons.
| Cell Experiment | |
|---|---|
| Cell lines | MDA-MB-231 and MDA-MB-435 cells |
| Preparation method | Inhibition of DNA synthesis assay. MDA-MB-231 and MDA-MB-435 cells were placed in 6-well culturedishes at 10,000 cells/well in 2 ml of medium. The following day, 5-AZA-CdR and depsi, alone or in combination, were added to thecells at the indicated concentrations. At 48 hr, 0.5μ Ci [3H]thymidine (6.7 Ci/mmol, ICN Biomedicals, Irvine, CA) was addedto the medium for an additional 24 hr. The cells were then rinsedwith PBS, trypsinized, suspended in a 0.9% NaCl solution, trans-ferred to a 25 mm diameter GF/C glass fiber filter and washed withcold 0.9% NaCl, 5% trichloroacetic acid and ethanol solutions.The dried filters were placed in EcoLite scintillation fluid (ICNBiomedicals) and the radioactivity incorporated into DNA wasmeasured with a scintillation counter. |
| Concentrations | 0~1000ng/ml |
| Incubation time | 24 hr |
| Animal Experiment | |
|---|---|
| Animal models | EJ6 human bladder cancer cell tumor-bearing athymic nu/nu mice |
| Formulation | PBS |
| Dosages | 5 mg/kg every 7 days for 25 days |
| Administration | subcutaneous (SQ) administration |
| Molecular Weight | 303.33 |
| Formula | C16H18FN3O2 |
| CAS Number | 150812-12-7 |
| Solubility (25°C) | DMSO 33 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related Potassium Channel Products |
|---|
| NPBA
NPBA is a potassium K2P channel TASK-3 (KCNK9) agonist and a tandem pore domain weak inward rectifier K+ channel (TWIK2) channel blocker. In addition, NPBA inhibits the activation of NLRP3 inflammasome in macrophages. |
| BeKm-1
BeKm-1 is a HERG (human ether-a-go-go-related gene) blocking compound. |
| Apamin
Apamin (Apamine) is a specifically selective blocker of Ca2+-activated K+ (SK) channels and exhibits anti-inflammatory and anti-fibrotic activity. |
| Phe-Met-Arg-Phe amide trifluoroacetate
Phe-Met-Arg-Phe amide trifluoroacetate is an activator of K+ current, with ED50 of 23 nM in the peptidergic caudodorsal neurons. |
| Iberiotoxin
Iberiotoxin is a toxin isolated from Buthus tamulus scorpion venom. |
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