Rufinamide (200 mg)
Rufinamide
CAS: 106308-44-5
Molecular Formula: C10H8F2N4O
Rufinamide (200 mg) - Names and Identifiers
| 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) |
Rufinamide (200 mg) - Physico-chemical Properties
| 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. |
Rufinamide (200 mg) - Risk and Safety
| 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 |
Rufinamide (200 mg) - Reference Information
| Use | Lufenamide is an antiepileptic triazole derivative that can reduce the discharge of sodium channel neurons. Used as an anticonvulsant, it is a neuroprotective and neuroresearch product. |
| antiepileptic drugs | Currently, lufiamide is still a new type of antiepileptic drug in my country. The English name is rufinamide. It is a triazole derivative. Its chemical structure is completely different from the existing antiepileptic drugs. Its mechanism of action is to regulate the cerebral voltage gate sodium ion channel. It was originally successfully developed by Eisai Company of the United States. It was approved by FDA on November 14, 2008. The trade name is BANZELTM. It is used in the adjuvant treatment of Lennox-Gastant syndrome (Lennox-Gastautsyndrome,LGS)-related seizures in children and adults aged 4 and above. lufenamide [CGP 33101, RUF331, Xilep TM] is a lead compound of 5-substituted-phenylalkyl-3-carbamoyl-4H-1, 2, 4-triazole compounds, with antispasmodic activity, currently developed by Novartis Switzerland as an antiepileptic drug. It was listed in the European Union in January 2007 and has entered the phase III clinical development phase in the United States. Phase II clinical development in Japan. Lufiamide has therapeutic benefits for local seizures and generalized tonic-clonic seizures (tonic-clonic seizure). It can be administered in combination or alone. Lufenamide is structurally unrelated to the already marketed epilepsy treatment drugs, and it mainly exerts its antispasmodic effect by limiting the ignition of neuronal sodium-dependent activity potential. Lufeamide has a wide treatment window, and patients with local or recurrent epilepsy who are tolerant to previous treatment still respond to Lufeamide. In addition to epilepsy, lufiamide is also undergoing phase II clinical development for the treatment of neuropathic pain. |
| biological activity | Rufinamide (CGP 33101) is a voltage-gated sodium channel blocker used as an anticonvulsant. |
| Target | Value |
Last Update：2024-04-09 20:48:19
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Product Name: Rufinamide Visit Supplier Webpage Request for quotationCAS: 106308-44-5
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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