Synonym
FCE-26742A; NW-1029; NW 1029; NW1029; PNU-0154339E; Priralfinamide; Ralfinamide.
IUPAC/Chemical Name
(2S)-2-(4-(2-Fluorobenzyloxy)benzylamino)propanamide
InChi Key
BHJIBOFHEFDSAU-LBPRGKRZSA-N
InChi Code
InChI=1S/C17H19FN2O2/c1-12(17(19)21)20-10-13-6-8-15(9-7-13)22-11-14-4-2-3-5-16(14)18/h2-9,12,20H,10-11H2,1H3,(H2,19,21)/t12-/m0/s1
SMILES Code
C[C@H](NCC1=CC=C(OCC2=CC=CC=C2F)C=C1)C(N)=O
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
Preparing Stock Solutions
The following data is based on the
product
molecular weight
302.35
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
1: Di Stefano AF, Radicioni MM, Rusca A. Pressor response to oral tyramine and monoamine oxidase inhibition during treatment with ralfinamide (NW-1029). Neurotox Res. 2013 May;23(4):315-26. doi: 10.1007/s12640-012-9344-5. Epub 2012 Aug 8. PubMed PMID: 22872464.
2: Bauer M, Bliesath H, Leuratti C, Lackner E, Dieterle W, Müller M, Brunner M. Disposition and metabolism of ralfinamide, a novel Na-channel blocker, in healthy male volunteers. Pharmacology. 2010;86(5-6):297-305. doi: 10.1159/000321322. Epub 2010 Nov 11. PubMed PMID: 21071997.
3: Browne LE, Clare JJ, Wray D. Functional and pharmacological properties of human and rat NaV1.8 channels. Neuropharmacology. 2009 Apr;56(5):905-14. doi: 10.1016/j.neuropharm.2009.01.018. Epub 2009 Jan 31. PubMed PMID: 19371587.
4: Zhang SH, Blech-Hermoni Y, Faravelli L, Seltzer Z. Ralfinamide administered orally before hindpaw neurectomy or postoperatively provided long-lasting suppression of spontaneous neuropathic pain-related behavior in the rat. Pain. 2008 Oct 15;139(2):293-305. doi: 10.1016/j.pain.2008.04.020. Epub 2008 Jun 25. PubMed PMID: 18583049.
5: Yamane H, de Groat WC, Sculptoreanu A. Effects of ralfinamide, a Na+ channel blocker, on firing properties of nociceptive dorsal root ganglion neurons of adult rats. Exp Neurol. 2007 Nov;208(1):63-72. Epub 2007 Jul 19. PubMed PMID: 17707373; PubMed Central PMCID: PMC2117901.
6: Bayes M, Rabasseda X, Prous JR. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2005 Jul-Aug;27(6):411-61. PubMed PMID: 16179960.
7: Bayés M, Rabasseda X, Prous JR. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2005 Mar;27(2):145-59. PubMed PMID: 15834466.
8: Stummann TC, Salvati P, Fariello RG, Faravelli L. The anti-nociceptive agent ralfinamide inhibits tetrodotoxin-resistant and tetrodotoxin-sensitive Na+ currents in dorsal root ganglion neurons. Eur J Pharmacol. 2005 Mar 14;510(3):197-208. PubMed PMID: 15763243.
9: Cattabeni F. Ralfinamide. Newron Pharmaceuticals. IDrugs. 2004 Oct;7(10):935-9. PubMed PMID: 15478019.