Raxatrigine HCl
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MedKoo CAT#: 326726

CAS#: 934240-31-0 (HCl)

Description: Raxatrigine, also known as vixotrigine, GSK1014802, and CNV1014802, is a small molecule state-dependent sodium channel blocker; Nav1.7 sodium channel inhibitor.


Chemical Structure

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Raxatrigine HCl
CAS# 934240-31-0 (HCl)

Theoretical Analysis

MedKoo Cat#: 326726
Name: Raxatrigine HCl
CAS#: 934240-31-0 (HCl)
Chemical Formula: C18H20ClFN2O2
Exact Mass: 0.00
Molecular Weight: 350.820
Elemental Analysis: C, 61.63; H, 5.75; Cl, 10.10; F, 5.42; N, 7.99; O, 9.12

Price and Availability

Size Price Availability Quantity
5mg USD 150 Ready to ship
10mg USD 250 Ready to ship
25mg USD 550 Ready to ship
50mg USD 950 Ready to ship
100mg USD 1450 Ready to ship
200mg USD 1850 Ready to ship
500mg USD 2650 Ready to ship
1g USD 3450 2 Weeks
2g USD 5950 2 Weeks
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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 hydrochloride; Vixotrigine;

IUPAC/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

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

More Info:

Biological target: Raxatrigine is a sodium channel blocker and a Nav1.7 sodium channel inhibitor.
In vitro activity: This study demonstrates that raxatrigine enhances the inactivation but does not reduce the activation of Nav1.7 channels. Reference: Acta Pharmacol Sin. 2018 Apr;39(4):587-596. https://pubmed.ncbi.nlm.nih.gov/29094728/
In vivo activity: Orally administered raxatrigine for neuropathic pain is well-tolerated when administered as single doses up to 825 mg and multiple doses up to 450 mg twice daily. Reference: Clin Transl Sci. 2021 Jul;14(4):1272-1279. https://pubmed.ncbi.nlm.nih.gov/33278330/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 31.0 88.40

Preparing Stock Solutions

The following data is based on the product molecular weight 350.82 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.

Recalculate based on batch purity %
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
Formulation protocol: 1. Hinckley CA, Kuryshev Y, Sers A, Barre A, Buisson B, Naik H, Hajos M. Characterization of Vixotrigine, a Broad-Spectrum Voltage-Gated Sodium Channel Blocker. Mol Pharmacol. 2021 Jan;99(1):49-59. doi: 10.1124/molpharm.120.000079. PMID: 33298520. 2. Zheng YM, Wang WF, Li YF, Yu Y, Gao ZB. Enhancing inactivation rather than reducing activation of Nav1.7 channels by a clinically effective analgesic CNV1014802. Acta Pharmacol Sin. 2018 Apr;39(4):587-596. doi: 10.1038/aps.2017.151. Epub 2017 Nov 2. PMID: 29094728; PMCID: PMC5888685. 3. Naik H, Steiner DJ, Versavel M, Palmer J, Fong R. Safety, Tolerability and Pharmacokinetics of Single and Repeat Doses of Vixotrigine in Healthy Volunteers. Clin Transl Sci. 2021 Jul;14(4):1272-1279. doi: 10.1111/cts.12935. Epub 2020 Dec 13. PMID: 33278330; PMCID: PMC8301589. 4. Witty DR, Alvaro G, Derjean D, Giblin GMP, Gunn K, Large C, Macpherson DT, Morisset V, Owen D, Palmer J, Rugiero F, Tate S, Hinckley CA, Naik H. Discovery of Vixotrigine: A Novel Use-Dependent Sodium Channel Blocker for the Treatment of Trigeminal Neuralgia. ACS Med Chem Lett. 2020 Jul 16;11(9):1678-1687. doi: 10.1021/acsmedchemlett.0c00263. PMID: 32945812; PMCID: PMC7488392.
In vitro protocol: 1. Hinckley CA, Kuryshev Y, Sers A, Barre A, Buisson B, Naik H, Hajos M. Characterization of Vixotrigine, a Broad-Spectrum Voltage-Gated Sodium Channel Blocker. Mol Pharmacol. 2021 Jan;99(1):49-59. doi: 10.1124/molpharm.120.000079. PMID: 33298520. 2. Zheng YM, Wang WF, Li YF, Yu Y, Gao ZB. Enhancing inactivation rather than reducing activation of Nav1.7 channels by a clinically effective analgesic CNV1014802. Acta Pharmacol Sin. 2018 Apr;39(4):587-596. doi: 10.1038/aps.2017.151. Epub 2017 Nov 2. PMID: 29094728; PMCID: PMC5888685.
In vivo protocol: 1. Naik H, Steiner DJ, Versavel M, Palmer J, Fong R. Safety, Tolerability and Pharmacokinetics of Single and Repeat Doses of Vixotrigine in Healthy Volunteers. Clin Transl Sci. 2021 Jul;14(4):1272-1279. doi: 10.1111/cts.12935. Epub 2020 Dec 13. PMID: 33278330; PMCID: PMC8301589. 2. Witty DR, Alvaro G, Derjean D, Giblin GMP, Gunn K, Large C, Macpherson DT, Morisset V, Owen D, Palmer J, Rugiero F, Tate S, Hinckley CA, Naik H. Discovery of Vixotrigine: A Novel Use-Dependent Sodium Channel Blocker for the Treatment of Trigeminal Neuralgia. ACS Med Chem Lett. 2020 Jul 16;11(9):1678-1687. doi: 10.1021/acsmedchemlett.0c00263. PMID: 32945812; PMCID: PMC7488392.

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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.