Rufinamide (CGP 33101; RUF 331)

Alias: E-2080; RUF-331; E2080; CGP-33101; RUF331; CGP 33101; E 2080; RUF 331; CGP33101; Trade names: BANZEL; Inovelon.
Cat No.:V1643 Purity: ≥98%
Rufinamide (also known as CGP-33101; E-2080; RUF-331; BANZEL; Inovelon)is a voltage-gated sodium channel blocker approved as an antiepilepic agent for seizure treatment.
Rufinamide (CGP 33101; RUF 331) Chemical Structure CAS No.: 106308-44-5
Product category: Sodium Channel
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
25mg
50mg
100mg
250mg
500mg
1g
Other Sizes

Other Forms of Rufinamide (CGP 33101; RUF 331):

  • Rufinamide-d2 (CGP 33101-d2; E 2080-d2; RUF 331-d2)
  • Rufinamide-15N,d2 (CGP 33101-15N,d2; E 2080-15N,d2; RUF 331-15N,d2)
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Rufinamide (also known as CGP-33101; E-2080; RUF-331; BANZEL; Inovelon) is a voltage-gated sodium channel blocker approved as an antiepilepic agent for seizure treatment. It is a board spectrum anticonvulsant that is used in combination with other medication and therapy to treat Lennox–Gastaut syndrome and various other seizure disorders. Rufinamide has efficacy for partial seizures. Rufinamide prolongs the inactivation of sodium channels and limits the frequency of action potential firing in cultured and acutely isolated neurons.

Biological Activity I Assay Protocols (From Reference)
ln Vitro

In vitro activity: Rufinamide is extensively metabolised by non-CYP450 systems with a half-life of 8-12 hours. Rufinamide’s mechanism of action is thought to be inhibition of sodium-dependent action potentials in neurons, with possible membrane-stabilising effects. Rufinamide hydrolysis is mediated primarily by human carboxylesterase (hCE) 1 and is nonsaturable up to 500 μM.

ln Vivo
Rufinamide given orally at 20 mg/kg every 12 h in healthy dogs should result in a plasma concentration and half-life sufficient to achieve the therapeutic level extrapolated from humans without short-term adverse effects in adult dogs. Rufinamide alleviates injury-induced mechanical allodynia for 4 hours. Rufinamide reduces peak current and stabilizes the inactivated state of voltage-gated sodium channel Nav1.7, with similar effects in dorsal root ganglion neurons in the Spared Nerve Injury neuropathic pain model in mice. Rufinamide suppresses pentylenetetrazol-induced seizures in mice (ED(50) 45.8 mg/kg) but not rats, and is active against MES-induced tonic seizures in mice (ED(50) 23.9 mg/kg) and rats (ED(50) 6.1 mg/kg). Rufinamide suppresses pentylenetetrazol-, bicuculline-, and picrotoxin-induced clonus in mice (ED(50) 54.0, 50.5, and 76.3 mg/kg, respectively). Rufinamide is partially effective in the mouse strychnine test.
Animal Protocol
20 mg/kg; oral
Dogs
References
Int J Clin Pract.2006Nov;60(11):1497-501;J Vet Pharmacol Ther.2012 Dec;35(6):529-33
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C10H8F2N4O
Molecular Weight
238.19
CAS #
106308-44-5
SMILES
O=C(C1=CN(CC2=C(F)C=CC=C2F)N=N1)N
InChi Key
POGQSBRIGCQNEG-UHFFFAOYSA-N
InChi Code
InChI=1S/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)
Chemical Name
1-(2,6-difluorobenzyl)-1H-1,2,3-triazole-4-carboxamide
Synonyms
E-2080; RUF-331; E2080; CGP-33101; RUF331; CGP 33101; E 2080; RUF 331; CGP33101; Trade names: BANZEL; Inovelon.
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 47 mg/mL (197.3 mM)
Water:<1 mg/mL
Ethanol:<1 mg/mL
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 4.1983 mL 20.9916 mL 41.9833 mL
5 mM 0.8397 mL 4.1983 mL 8.3967 mL
10 mM 0.4198 mL 2.0992 mL 4.1983 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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