Retigabine

Product details

• Chemical name: Ethyl N-[2-amino-4-[(4-fluorophenyl)methylamino]phenyl]carbamate.
• Also known as: D-23129, Ezogabine, Trobalt®, Potiga®
• CAS number: 150812-12-7
• Molecular formula: C16H18FN3O2.
• Purity: >99% (HPLC)
• Concentration: 0.1-100 µM.
• Form: Lyophilized Powder
• Solubility: DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
• Reconstitution: Centrifuge the vial before adding solvent (10,000 x g for 5 minutes) to spin down all the powder to the bottom of the vial. The lyophilized product may be difficult to visualize. Add solvent directly to the centrifuged vial. Tap the vial to aid in dissolving the lyophilized product. Tilt and gently roll the liquid over the walls of the vial. Avoid vigorous vortexing. Light vortexing for up to 3 seconds is acceptable if needed. The product is soluble in pure water at high micromolar concentrations (100 µM - 1 mM). For long-term storage in solution, we recommend preparing a stock solution by dissolving the product in double-distilled water (ddH2O) at a concentration between 100-1000x of the final working concentration. Divide the stock solution into small aliquots and store at -20°C. Before use, thaw the relevant vial(s) and dilute to the desired working concentration in your working buffer. Centrifuge all product preparations before use. It is recommended to prepare fresh solutions in working buffers just before use. Avoid multiple freeze-thaw cycles to maintain biological activity
• Shipping: Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
• Target: KCNQ2, KCNQ3, and KCNQ4 K+ channels
• Source: Synthetic
• Activity: Retigabine is a potent and selective KCNQ (KV7, M-) channel modulator (enhancer)1-4, which is used in the clinic to treat epilepsy5. Retigabine (0.1 to 10 μM) induced a K+ current and hyperpolarized CHO cells expressing KV7.2/3 cells2 as well as other channels in the following order: KV7.3 > KV7.2/3 > KV7.2 > KV7.43. Similar effects were seen with 10 μM retigabine in oocytes expressing the KV7.2/3 heteromeric channel4.
• Alternative names: D-23129, Ezogabine, Trobalt®, Potiga®

Scientific background

The KCNQ family of voltage-gated K+ channels includes five known members: KCNQ1 to KCNQ5. Structurally, the KCNQ family belongs to the six transmembrane domain category of K+ channels. KCNQ family members can form either homomultimeric or heteromultimeric channels with different functional consequences. For example, KCNQ2 and KCNQ3 heteromultimers give rise to a much larger channel current than when either protein is expressed alone. Indeed, KCNQ2/KCNQ3 heteromultimers are believed to be the molecular correlates of the so-called M current. This current is a K+ neuronal current that is strongly inhibited by the activation of the M1 subtype of the muscarinic acetylcholine receptor. Mutations in either KCNQ2 or KCNQ3 are associated with a form of epilepsy known as benign familial neonatal convulsions (BNFC)1-3.Retigabine is a potent and selective KCNQ (KV7, M-) channel modulator (enhancer)4-7, which is used in the clinic to treat epilepsy8. Retigabine (0.1 to 10 µM) induced a K+ current and hyperpolarized CHO cells expressing KV7.2/3 cells5 as well as other channels in the following order: KV7.3 > KV7.2/3 > KV7.2 > KV7.46. Similar effects were seen with 10 µM retigabine in oocytes expressing the KV7.2/3 heteromeric channel7.

Lead time: 1-2 Business Days

Country of origin: Israel/IL

Applications key

Application key: FC- Flow cytometry, IFC- Indirect flow cytometry, IHC- Immunohistochemistry,LCI- Live cell imaging, Calcium imaging assay,Cell survival assay, Electrophysiology, Neurite outgrowth assay.

Bioassay tested: Yes

Cited application(s)

Electrophysiology

• SDS (PDF)

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