Rufinamide(CGP 33101 RUF 331)

Molecular Weight (MW)	238.19
Formula	C10H8F2N4O
CAS No.	106308-44-5
Storage	-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)	DMSO: 47 mg/mL (197.3 mM)
Water:<1 mg/mL
Ethanol:<1 mg/mL
Other info	Chemical Name: 1-(2,6-difluorobenzyl)-1H-1,2,3-triazole-4-carboxamide 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) SMILES Code: O=C(C1=CN(CC2=C(F)C=CC=C2F)N=N1)N
Synonyms	E-2080; RUF-331; E2080; CGP-33101; RUF331; CGP 33101; E 2080; RUF 331; CGP33101; Trade names: BANZEL; Inovelon.

Molecular Weight (MW)

238.19

Formula

C10H8F2N4O

CAS No.

106308-44-5

Storage

-20℃ for 3 years in powder form

-80℃ for 2 years in solvent

Solubility (In vitro)

DMSO: 47 mg/mL (197.3 mM)

Water:<1 mg/mL

Ethanol:<1 mg/mL

Other info

Chemical Name: 1-(2,6-difluorobenzyl)-1H-1,2,3-triazole-4-carboxamide

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)

SMILES Code: O=C(C1=CN(CC2=C(F)C=CC=C2F)N=N1)N

Synonyms

E-2080; RUF-331; E2080; CGP-33101; RUF331; CGP 33101; E 2080; RUF 331; CGP33101; Trade names: BANZEL; Inovelon.

In 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.
In 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 model	Dogs
Formulation & Dosage	20 mg/kg; oral
References	Int J Clin Pract. 2006 Nov;60(11):1497-501; J Vet Pharmacol Ther. 2012 Dec;35(6):529-33

In 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.

In 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 model

Dogs

Formulation & Dosage

20 mg/kg; oral

References

Int J Clin Pract. 2006 Nov;60(11):1497-501; J Vet Pharmacol Ther. 2012 Dec;35(6):529-33

CAS NO:	106308-44-5
规格:	≥98%

包装	价格(元)
5mg	电议
10mg	电议
25mg	电议
50mg	电议
100mg	电议
250mg	电议
500mg	电议
1g	电议