Raxatrigine - 99%, high purity , Sodium channel protein type IX alpha subunit blocker, CAS No.934240-30-9, Sodium channel protein type IX alpha subunit blocker

  • ≥99%
Item Number
R649384
Grouped product items
SKUSizeAvailabilityPrice Qty
R649384-1mg
1mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$85.90
R649384-5mg
5mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$180.90
R649384-10mg
10mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$288.90

Basic Description

SynonymsN-{2-oxo-2-[(3S)-3-{[(1s,4s)-4-hydroxy-4-[5-(pyrimidin-2-yl)pyridin-2-yl]cyclohexyl]amino}pyrrolidin-1-yl]ethyl}-3-(trifluoromethyl)benzamide | DB11706 | 2,6-Nonadienoic acid, 7-ethyl-9-[(2R,3S)-3-ethyl-3-methyloxiranyl]-3-methyl-, methyl ester, (2E,6E)-
Specifications & Purity≥99%
Biochemical and Physiological MechanismsRaxatrigine (GSK-1014802) is a novel small molecule state-dependent sodium channel blocker; Nav1.7 sodium channel inhibitor .
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
Action TypeBLOCKER
Mechanism of actionSodium channel protein type IX alpha subunit blocker
Product Description

Raxatrigine (GSK-1014802) is a novel small molecule state-dependent sodium channel blocker; Nav1.7 sodium channel inhibitor .

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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Form:Solid

IC50& Target:Sodium channel blocker

Product Properties

ALogP2.4

Associated Targets(Human)

SCN10A Tclin Sodium channel protein type 10 subunit alpha (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
SCN4A Tclin Sodium channel protein type 4 subunit alpha (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
SCN1A Tclin Sodium channel protein type I alpha subunit (483 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SCN5A Tclin Sodium channel protein type V alpha subunit (3462 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SCN7A Tclin Sodium channel protein type VII alpha subunit (136 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Scn2a Sodium channel protein type II alpha subunit (191 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Scn3a Sodium channel protein type III alpha subunit (24 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Scn9a Sodium channel protein type IX alpha subunit (69 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Scn8a Sodium channel protein type VIII alpha subunit (53 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Scn10a Sodium channel protein type X alpha subunit (425 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Scn4a Sodium channel protein type IV alpha subunit (55 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Names and Identifiers

IUPAC Name (2S,5R)-5-[4-[(2-fluorophenyl)methoxy]phenyl]pyrrolidine-2-carboxamide
INCHI 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
InChi Key JESCETIFNOFKEU-SJORKVTESA-N
Canonical SMILES C1CC(NC1C2=CC=C(C=C2)OCC3=CC=CC=C3F)C(=O)N
Isomeric SMILES C1C[C@H](N[C@H]1C2=CC=C(C=C2)OCC3=CC=CC=C3F)C(=O)N
Alternate CAS 934240-30-9
PubChem CID 16046068
MeSH Entry Terms BIIB074;CNV1014802;raxatrigine;vixotrigine
Molecular Weight 314.4

Certificates

Certificate of Analysis(COA)

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Chemical and Physical Properties

SolubilityDMSO : 83 mg/mL (264.04 mM; Need ultrasonic and warming)

Related Documents

Solution Calculators