| Name | Raxatrigine |
| Description | Raxatrigine (CNV 1014802) has been investigated for the treatment of Bipolar Disorder and Bipolar Depression. |
| Kinase Assay | Binding or activity of EVP-6124 is measured at 10 μM in a selectivity panel according to standard validated protocols under conditions defined by the contractor. For the 5-HT2A receptor binding assay, membranes are prepared from HEK293 cellsexpressing the human recombinant 5-HT2A receptor. For 5-HT2B and 5-HT2C receptor binding assays, membranes are prepared from CHO cells expressing the human recombinant 5-HT2B or 5-HT2C receptor. Affinity is determined by incubating different concentrations of EVP-6124 in binding buffer for 1 h. For 5-HT2A binding, the incubation is at 22°C in the presence of 0.5 nM [3H]-ketanserin; for 5-HT2B, at 22°C in the presence of 2 nM [3H]-mesulergine; and for 5-HT2C, at 37°C in the presence of 1 nM [3H]-mesulergine. Nonspecific binding is determined in the presence of 1 μM ketanserin, 10 μM mesulergine, or 10 μM RS-102221 for 5-HT2A, 5-HT2B, or 5-HT2C, respectively. All measurements are performed in triplicate. EVP-6124 is also tested in the 5-HT2B rat gastric fundus tissue response assay. Briefly, inhibition of α-methyl serotonin-induced contraction is isometrically measured. All measurements are performed in duplicate[1]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (6.36 mM), Sonication is recommended.
DMSO : 50 mg/mL (159.06 mM), Sonication is recommended.
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| Keywords | SodiumChannel | Sodium Channel | Raxatrigine | Na+ channels | Na channels | Inhibitor | inhibit | GSK1014802 | GSK 1014802 |
| Inhibitors Related | Phenytoin sodium | Procaine | Ranolazine dihydrochloride | Tetracaine hydrochloride | Lidocaine | Safinamide | Permethrin | Valproic Acid | L-Aspartic aicd sodium | Lidocaine hydrochloride | Mebeverine hydrochloride | Dibucaine |
| Related Compound Libraries | Pain-Related Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Neuroprotective Compound Library | Inhibitor Library | Anti-Cardiovascular Disease Compound Library | Bioactive Compounds Library Max | Fluorochemical Library | Ion Channel Targeted Library | Anti-Cancer Drug Library |
United States
