WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 510347
CAS#: 934240-30-9 (free base).
Description: Raxatrigine, also known as GSK1014802 and CNV-1014802, is a sodium channel antagonist that is currently in phase II studies in bipolar depression. CNV1014802 is a peripherally and centrally acting agent that inhibits sodium channels in a state-dependent fashion. CNV1014802 shows selectivity for the Nav1.7 subtype over the other subtypes tested (Nav1.1, Nav1.2, Nav1.3, Nav1.5, Nav1.6 and TTX-R), for both the resting and depolarized states.
MedKoo Cat#: 510347
Name: Raxatrigine free base
CAS#: 934240-30-9 (free base).
Chemical Formula: C18H19FN2O2
Exact Mass: 314.14306
Molecular Weight: 314.36
Elemental Analysis: C, 68.77; H, 6.09; F, 6.04; N, 8.91; O, 10.18
Related CAS #: 934240-31-0 (HCl) 934240-30-9 (free base) 934240-35-4 (mesylate)
Synonym: GSK1014802; GSK 1014802; GSK-1014802; CNV1014802; CNV-1014802; CNV 1014802; Raxatrigine; Raxatrigine free base; Vixotrigine;
IUPAC/Chemical Name: (2S,5R)-5-(4-((2-fluorobenzyl)oxy)phenyl)pyrrolidine-2-carboxamide
InChi Key: JESCETIFNOFKEU-SJORKVTESA-N
InChi Code: InChI=1S/C18H19FN2O2/c19-15-4-2-1-3-13(15)11-23-14-7-5-12(6-8-14)16-9-10-17(21-16)18(20)22/h1-8,16-17,21H,9-11H2,(H2,20,22)/t16-,17+/m1/s1
SMILES Code: O=C(N)[C@H]1N[C@@H](C2=CC=C(OCC3=CC=CC=C3F)C=C2)CC1
Appearance: Solid powder
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, not in water
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
The following data is based on the product molecular weight 314.36 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: Deuis JR, Wingerd JS, Winter Z, Durek T, Dekan Z, Sousa SR, Zimmermann K,
Hoffmann T, Weidner C, Nassar MA, Alewood PF, Lewis RJ, Vetter I. Analgesic
Effects of GpTx-1, PF-04856264 and CNV1014802 in a Mouse Model of NaV1.7-Mediated
Pain. Toxins (Basel). 2016 Mar 17;8(3). pii: E78. doi: 10.3390/toxins8030078.
PubMed PMID: 26999206; PubMed Central PMCID: PMC4810223.
2: Bagal SK, Chapman ML, Marron BE, Prime R, Storer RI, Swain NA. Recent progress
in sodium channel modulators for pain. Bioorg Med Chem Lett. 2014 Aug
15;24(16):3690-9. doi: 10.1016/j.bmcl.2014.06.038. Epub 2014 Jun 21. Review.
PubMed PMID: 25060923.
3: Zakrzewska JM, Palmer J, Ettlin DA, Obermann M, Giblin GM, Morisset V, Tate S,
Gunn K. Novel design for a phase IIa placebo-controlled, double-blind randomized
withdrawal study to evaluate the safety and efficacy of CNV1014802 in patients
with trigeminal neuralgia. Trials. 2013 Nov 23;14:402. doi:
10.1186/1745-6215-14-402. PubMed PMID: 24267010; PubMed Central PMCID:
PMC4222641.
Related CAS#
CAS#934240-31-0 ( Raxatrigine hydrochloride)
CAS#934240-30-9 ( Raxatrigine free).
