Name | Rufinamide |
Synonyms | E 2080 Inovelon CGP 33101 Rufinamide RufinaMide(Banzel) Rufinamide (200 mg) 1-(2,6-Difluorobenzyl)-1H-1,2,3-triazole-4-carboxamide 1H-1,2,3-TRIAZOLE-4-CARBOXAMIDE, 1-[(2,6-DIFLUOROPHENYL)METHYL]- |
CAS | 106308-44-5 |
EINECS | 200-659-6 |
InChI | InChI=1/C10H8F2N4O/c11-7-2-1-3-8(12)6(7)4-16-5-9(10(13)17)14-15-16/h1-3,5H,4H2,(H2,13,17) |
Molecular Formula | C10H8F2N4O |
Molar Mass | 238.19 |
Density | 1.52±0.1 g/cm3(Predicted) |
Melting Point | 232-234?C |
Boling Point | 473.8±55.0 °C(Predicted) |
Flash Point | 2℃ |
Solubility | 25°C: DMSO 48mg/mL; Water <1 mg/mL; Ethanol <1 mg/mL |
Vapor Presure | 3.81E-09mmHg at 25°C |
Appearance | White powder |
Color | white |
Merck | 14,8293 |
pKa | 14.37±0.50(Predicted) |
Storage Condition | -20°C |
Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month. |
Refractive Index | 1.634 |
MDL | MFCD00865314 |
Physical and Chemical Properties | Storage Conditions:? 20 ℃ |
In vitro study | Rufinamide is extensively metabolized by non-CYP450 systems with a half-life of 8-12 hours. The mechanism of Rufinamide is thought to be the inhibition of sodium-dependent action potentials in neurons, possibly with a membrane stabilizing effect. Rufinamide hydrolysis is mainly mediated by human carboxylesterase (esterase hCE)1 and saturates at concentrations up to 500 μm. |
In vivo study | In adult dogs, Rufinamide, given orally at 20 mg/kg every 12 hours, results in plasma concentrations and half-life sufficient to reach therapeutic levels without short-term adverse effects. Rufinamide attenuates injury-induced mechanical allodynia for 4 hours. In mice, Rufinamide reduced peak currents and stabilized voltage-gated sodium channel Nav1.7 inactivation, with similar effects on dorsal root ganglion neurons in a neuropathic pain model of sciatic nerve branch injury in mice. Rufinamide inhibits pentylenetetrazol-induced seizures in mice (ED(50)45.8 mg/kg), but not in rats, and is effective against MES-induced tonic seizures in mice (ED(50)23.9 mg/kg) and rats (ED(50)6.1 mg/kg). Rufinamide inhibits pentyleneetrazol-,bicuculline-, and picrotoxin-induced clonus in mice (ED(50)54.0,50.5, and 76.3 mg/kg). Rufinamide is a partially valid rat strychnine test. |
Risk Codes | R11 - Highly Flammable R23/24/25 - Toxic by inhalation, in contact with skin and if swallowed. R39/23/24/25 - R48 - Danger of serious damage to health by prolonged exposure R41 - Risk of serious damage to eyes R38 - Irritating to the skin R28 - Very Toxic if swallowed |
Safety Description | S7 - Keep container tightly closed. S16 - Keep away from sources of ignition. S36/37 - Wear suitable protective clothing and gloves. S45 - In case of accident or if you feel unwell, seek medical advice immediately (show the label whenever possible.) S36/37/39 - Wear suitable protective clothing, gloves and eye/face protection. S28 - After contact with skin, wash immediately with plenty of soap-suds. S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S24/25 - Avoid contact with skin and eyes. |
UN IDs | UN 1648 3 / PGII |
WGK Germany | 3 |
HS Code | 29339900 |