MedKoo Biosciences

Raxatrigine free base
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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 vixotrigine, GSK1014802, and CNV1014802, is a small molecule state-dependent sodium channel blocker; Nav1.7 sodium channel inhibitor.

Chemical Structure

Raxatrigine free base

CAS# 934240-30-9 (free base)

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 510347
Name: Raxatrigine free base
CAS#: 934240-30-9 (free base)
Chemical Formula: C18H19FN2O2
Exact Mass: 314.14
Molecular Weight: 314.360
Elemental Analysis: C, 68.77; H, 6.09; F, 6.04; N, 8.91; O, 10.18

Price and Availability

Size	Price	Availability	Quantity
10mg	USD -2
25mg	USD -2
50mg	USD 950
100mg	USD 1450
200mg	USD 2150
500mg	USD 2950
1g	USD 3750
2g	USD 5650
5g	USD 9950
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

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

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

Product Data:

Product Data

Instruction:

View handling instruction

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	83.0	264.04

Preparing Stock Solutions

The following data is based on the product molecular weight 314.360000000000000000000000000000 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

Formulation protocol:	1. 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. 2. 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. 3. 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. 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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*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

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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.

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Raxatrigine free base featured