Raxatrigine (GSK1014802)
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    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.


Price and Availability

Size
Price

10mg
Not available
100mg
USD 1450
1g
USD 3750
Size
Price

25mg
Not available
200mg
USD 2150
2g
USD 5650
Size
Price

50mg
USD 950
500mg
USD 2950
5g
USD 9950

GSK1014802 (Raxatrigine), purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received. Delivery time: overnight (USA/Canada); 3-5 days (worldwide). Shipping fee: from $30.00 (USA); from $45.00 (Canada); from $70.00 (international).


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 510347
Name: Raxatrigine (GSK1014802)
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).  

Synonym: GSK1014802; GSK 1014802; GSK-1014802; CNV1014802; CNV-1014802; CNV 1014802; Raxatrigine.

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


Technical Data

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).

Harmonized System Code:
293490


Additional Information

  Related CAS#
CAS#934240-31-0 ( Raxatrigine hydrochloride)
CAS#934240-30-9 ( Raxatrigine free).
 
 
 


References

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.