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Home / Biochemicals / Small Molecules

Ralfinamide mesylate

SKU : BHB21300301

A Use-Dependent Blocker of NaV Channels

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Mfr.No.	R-105, R-105_10 mg, R-105_25 mg, R-105_5 mg, R-105_50 mg
Description	Ralfinamide mesylate (#R-105) is a highly pure, synthetic, and biologically active compound.
Molecular Formula	C18H23FN2O5SCH3SO3H.
Synonyms	Synthetic
Background	Voltage-gated Na+ channels (VGSCs) comprise a large multi-gene family encoding individual subtypes that can be differentiated on the basis of primary structure, biophysical properties and sensitivity to the neurotoxin tetrodotoxin1-2. Most VGSCs, termed TTX-sensitive (TTXs), have been both found in brain and sensory neurons where they have a low threshold for activation and rapid inactivation kinetics; by contrast other VGSCs are termed TTX-resistant (TTXr). These may play a key role in persistent pain states, including neuropathic and chronic inflammatory pain.Ralfinamide mesylate (NW-1029) is a Na+ channel blocker that suppresses tetrodotoxin (TTX)-resistant Na+ currents in small to medium size (C-type) dorsal root ganglia (DRG) neurons about twice as selectively as it blocks TTX-sensitive currents in the same neurons; IC50 values for tonic block of half-maximal inactivated tetrodotoxin-resistant and tetrodotoxin-sensitive currents are 10 uM and 22 uM, respectively3. The blocking action of ralfinamide shows frequency and voltage dependence3. In experimental animal models of inflammatory and neuropathic pain, systemic administration of ralfinamide elicits anti-nociceptive effects4-6.
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	10-200 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	202825-45-4
Molecular Weight	398.5
Solubility	DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
Target	NaV Na+ channels
Activity	Ralfinamide mesylate is a Na+ channel blocker1. Its IC50 values for tonic block of half-maximal inactivated tetrodotoxin (TTX)-resistant and TTX-sensitive currents are 10 and 22 uM, respectively1. Ralfinamide displays analgesic effects in animal models of inflammatory and neuropathic pain2.
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: (2S)-2-(((4-((2-Fluorophenyl) methoxy)phenyl)methyl)amino)-propanamide methanesulfonate.

Purity	>99%
Form	Lyophilized Powder
Storage	Storage of solutions: Up to four weeks at 4°C or three months at -20°C.

Product Manual	SDS

Reference	Zimmermann, M. et al. (2001) Eur. J. Phamacol. 429, 23. Goldin, A. L. et al. (2001) Annu. Rev. Physiol 63, 871. Stummann, T. C. et al. (2005) Eur. J. Pharmacol. 510, 197. Veneroni, O. et al. (2003) Pain. 102, 17. Zhang, S. H. et al. (2008) Pain 139, 293. Yamane, H. et al. (2007) Exp. Neurol. 208, 63. Stummann, T.C. et al. (2005) Eur. J. Pharmacol. 510, 197. Veneroni, O. et al. (2003) Pain. 102, 17.

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Combination SKU	Supplier No.	Size	Your price	Quantity
BHB21300301-1	R-105_10 mg	10 mg	$129		Add to Cart
BHB21300301-2	R-105_25 mg	25 mg	$243		Add to Cart
BHB21300301-3	R-105_5 mg	5 mg	$91		Add to Cart
BHB21300301-4	R-105_50 mg	50 mg	$429		Add to Cart

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