An inhibitor of voltage-gated sodium channels (IC50s = 22

Raxatrigine (hydrochloride) – 1 mg

Brand:
Cayman
CAS:
934240-31-0
Storage:
-20
UN-No:
Non-Hazardous - /

Raxatrigine is an inhibitor of voltage-gated sodium channels (Nav; IC50s = 22, 13, 23, 10, 84, 15, 32, and 6 µM for Nav1.1-Nav1.8 channels in a FLIPR membrane potential assay using HEK293 cells).{38414} Its activity is state-dependent at the Nav1.7 channel, with a nine-fold increase in potency for the open/inactivated state (IC50 = 6.3 µM) compared to the closed/resting state (IC50 = 54 µM). Raxatrigine (30 mg/kg, i.p.) decreases spontaneous pain behavior in an OD1 mouse pain model. Formulations containing raxatrigine have been investigated in clinical trials for the treatment of trigeminal neuralgia and lumbosacral radiculopathy (sciatica).  

 

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SKU: 23490 - 1 mg Category:

Description

An inhibitor of voltage-gated sodium channels (IC50s = 22, 13, 23, 10, 84, 15, 32, and 6 µM for Nav1.1- Nav1.8 channels); has state-dependent activity at the Nav1.7 channel (IC50s = 6.3 and 54 µM for open/inactivated and closed/resting states); decreases pain behavior in an OD1 mouse pain model

Formal name: (2S)-5R-[4-[(2-fluorophenyl)methoxy]phenyl]-2-pyrrolidinecarboxamide, monohydrochloride

Synonyms:  GSK1014802A

Molecular weight: 350.8

CAS: 934240-31-0

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Ion Channel Modulation|Blockers||Research Area|Neuroscience|Pain Research

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