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Home / Biochemicals / Small Molecules

Retigabine dihydrochloride

SKU : BHB21300300

A Potent and Selective Modulator of KCNQ Channels

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Mfr.No.	R-101, R-101_10 mg, R-101_100 mg, R-101_25 mg, R-101_250 mg, R-101_50 mg
Description	Retigabine dihydrochloride (#R-101) is a highly pure, synthetic, and biologically active compound.
Molecular Formula	C16H20Cl2FN3O2.
Synonyms	Synthetic
Background	The KCNQ family of voltage-gated K+ channels includes 5 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 uM) 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 uM retigabine in oocytes expressing the KV7.2/3 heteromeric channel7.
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
Concentration	0.1-100 uM
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 uM - 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
Cas Number	150812-13-8
Molecular Weight	376.2
Solubility	Water. Centrifuge all product preparations before use (10000 x g 5 min).
Target	KCNQ2, KCNQ3, KCNQ4 K+ channels
Activity	Retigabine is a potent and selective KCNQ (KV7, M-) channel modulator (enhancer)1.
Country Of Origin	Israel/IL
UNSPSC Code	41116134
Application	FC- Flow cytometry, IFC- Indirect flow cytometry, IHC- Immunohistochemistry,LCI- Live cell imaging, Calcium imaging assay,Cell survival assay, Electrophysiology, Neurite outgrowth assay
Lead Time	1-2 Business Days
Notes	Bioassay Tested: Yes Chemical Name: Ethyl N-(2-amino-4-((4-fluorophenyl)methylamino)phenyl)carbamate dihydrochloride.

Purity	>98%
Form	Lyophilized Powder
Storage	Storage After Reconstitution: The reconstituted solution can be stored at 4°C for up to 1 week. For longer periods (up to 6 months), small aliquots should be stored at -20°C. We do not recommend storing the product in working solutions for longer than a few days. Avoid multiple freeze-thaw cycles. Storage of solutions: Up to four weeks at 4°C or three months at -20°C.

Product Manual	SDS

Reference	Kullmann, D.M. (2002) Brain 125, 1117. Robbins, J. (2001) Pharmacol. Ther. 90, 1. Wang, H.S. et al. (1998) Science 282, 1890. Rundfeldt, C. (1997) Eur. J. Pharmacol. 336, 243. Wickenden, A.D. et al. (2000) Mol. Pharmacol. 58, 591. Tatulian, L. et al. (2001) J. Neurosci. 21, 5535. Main, M.J. et al. (2000) Mol. Pharmacol. 58, 253. Brodie, M.J. et al. (2010) Neurology 75, 1817. Main, M.J. et al. (2000) Mol. Pharmacol. 58, 253.

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Combination SKU	Supplier No.	Size	Your price	Quantity
BHB21300300-1	R-101_10 mg	10 mg	$57		Add to Cart
BHB21300300-2	R-101_100 mg	100 mg	$266		Add to Cart
BHB21300300-3	R-101_25 mg	25 mg	$92		Add to Cart
BHB21300300-4	R-101_250 mg	250 mg	$595		Add to Cart
BHB21300300-5	R-101_50 mg	50 mg	$151		Add to Cart

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