CNV1014802 hydrochloride

Cas：934240-31-0

Product Information：

CNV1014802 hydrochloride is a novel analgesic under development by Convergence Pharmaceuticals for the treatment of lumbosacral radiculopathy (sciatica) and trigeminal neuralgia (TGN). It acts as a selective, small-molecule, state-dependent Nav1.7 voltage-gated sodium channel blocker.

Chemical Formula: C18H20ClFN2O2

Molecular Weight: 350.8184

Elemental Analysis: C, 61.63; H, 5.75; Cl, 10.10; F, 5.42; N, 7.99; O, 9.12

Synonym:

GSK1014802

GSK 1014802

GSK-1014802

CNV1014802

CNV-1014802

CNV 1014802

Raxatrigine

Raxatrigine hydrochloride

Vixotrigine

Chemical Name: 

(2S,5R)-5-(4-((2-fluorobenzyl)oxy)phenyl)pyrrolidine-2-carboxamide hydrochloride

InChi Key: 

HEPUBAGOKRIZEO-PPPUBMIESA-N

InChi Code: 

InChI=1S/C18H19FN2O2.ClH/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);1H/t16-,17+;/m1./s1

Smiles Code:

O=C([C@H]1N[C@@H](C2=CC=C(OCC3=CC=CC=C3F)C=C2)CC1)N.[H]Cl

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).

HS Tariff Code: 2934.99.9001

In Vitro:

Like lamotrigine, both GSK2 and GSK3 were able to prevent the deficit in reversal learning produced by PCP, thus confirming their potential in the treatment of cognitive symptoms of schizophrenia. However, higher doses than those required for anticonvulsant efficacy of the drugs were needed for activity in the reversal-learning model, suggesting a lower therapeutic window relative to mechanism-dependent central side effects for this indication. Raxatrigine (GSK-1014802) received orphan-drug designation from the US Food and Drug Administration in July 2013.

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.

Products are for research use only. Not for human use.