[CAS NO. 934240-30-9] Raxatrigine
PRODUCTS SPECIFICATIONS [934240-30-9]
DESCRIPTION [934240-30-9]
Overview
| MDL | MFCD22580419 |
|---|---|
| Molecular Weight | 314.35 |
| Molecular Formula | C18H19FN2O2 |
| SMILES | O=C([C@H]1N[C@@H](C2=CC=C(OCC3=CC=CC=C3F)C=C2)CC1)N |
Summary
Raxatrigine (GSK-1014802) is a novel small molecule state-dependent sodium channel blocker; Nav1.7 sodium channel inhibitor .
IC50 & Target
Sodium channel blocker [1] .
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.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT00955396 | Biogen |
Healthy Volunteer
|
July 31, 2009 | Phase 1 |
| NCT02551497 | Biogen |
Healthy
|
April 30, 2015 | Phase 1 |
| NCT00964288 | Biogen |
Pain, Neuropathic|Neuropathic Pain
|
July 31, 2009 | Phase 1 |
| NCT01561027 | Biogen |
Lumbosacral Radiculopathy
|
April 30, 2011 | Phase 2 |
| NCT02359344 | Biogen |
Trigeminal Neuralgia
|
February 3, 2015 | Phase 1 |
| NCT00908154 | Biogen |
Bipolar Depression|Bipolar Disorder
|
May 31, 2008 | Phase 1 |
| NCT01540630 | Biogen |
Trigeminal Neuralgia
|
March 31, 2012 | Phase 2 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 83 mg/mL ( 264.04 mM ; Need ultrasonic and warming)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.1812 mL | 15.9058 mL | 31.8117 mL |
| 5 mM | 0.6362 mL | 3.1812 mL | 6.3623 mL |
| 10 mM | 0.3181 mL | 1.5906 mL | 3.1812 mL |
Synonyms
