| Identification | Back Directory | [Name]
GSK1014802 | [CAS]
934240-30-9 | [Synonyms]
CS-657
BIIB074)
GSK1014802
CNV1014082
Raxatrigine
CNV-1014802
Vixotrigine
MFCD22580419
GSK1014802(CNV1014802)
Raxatrigine (GSK1014802)
CNV1014802
(GSK-1014802
Melphalan Flufenamide Hydrochloride
CNV-1014802;RAXATRIGINE;VIXOTRIGINE;BIIB074
CNV1014802;GSK-1014802;GSK-1014802;RAXATRIGINE
(R)-5-{4-[(2-Fluorobenzyl)oxy]phenyl}-L-prolinamide
(5R)-5-{4-[(2-Fluorobenzyl)oxy]phenyl}-L-prolinamide
(5R)-5-(4-{[(2-fluorophenyl)methyl]oxy}phenyl)-L-prolinamide
(5R)-5-(4-{[(2-fluorophenyl)methyl]oxy}phenyl)-L-prolinamide-HCL
(2S,5R)-5-[4-[(2-Fluorophenyl)methoxy]phenyl]-2-pyrrolidinecarboxamide
2-Pyrrolidinecarboxamide, 5-[4-[(2-fluorophenyl)methoxy]phenyl]-, (2S,5R)- | [Molecular Formula]
C18H19FN2O2 | [MDL Number]
MFCD22580419 | [MOL File]
934240-30-9.mol | [Molecular Weight]
314.35 |
| Chemical Properties | Back Directory | [Boiling point ]
529.5±50.0 °C(Predicted) | [density ]
1.226±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
Powder | [pka]
16.16±0.40(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
Raxatrigine is used in the novel design for a phase IIa placebo-controlled, double-blind randomized withdrawal study to evaluate the safety and efficacy of CNV1014802 (novel sodium channel blocker) in patients with trigeminal neuralgia (unilateral facial discomfort). | [Biological Activity]
gsk1014802 (cnv1014802) is a novel sodium channel blocker [1][2][3].voltage-gated sodium channels (navs) are transmembrane ion channel proteins, which are involved in na+ ion conduction across cell membranes during cell membrane depolarization [2].gsk1014802 (cnv1014802) is a novel sodium channel blocker and is an effective anticonvulsant agent. in rats, gsk1014802 (20 - 80 mg/kg p.o.) attenuated the deficit in reversal learning induced by phencyclidine (pcp) in a dose-dependent way, which suggested the potential of gsk1014802 in the treatment of cognitive symptoms of schizophrenia. gsk2 was also a potent inhibitor of human mao-b with pic50 value of 7.96 but did not inhibit human mao-a. gsk2 inhibited rat forebrain mao-b with pki value of 7.20 [1]. cnv1014802 inhibited sodium channels in a state-dependent way. cnv1014802 exhibited selectivity for the nav1.7 subtype over the other subtypes (nav1.1, nav1.2, nav1.3, nav1.5, nav1.6 and ttx-r) [2].gsk1014802 had completed phase ii trials for lumbosacral radiculopathy and was in phase ii trials for trigeminal neuralgia (tn). furthermore, cnv1014802 was granted orphan drug designation in 2013 by fda for the treatment of trigeminal neuralgia [3]. | [storage]
Store at -20°C | [References]
[1]. large ch, bison s, sartori i, et al. the efficacy of sodium channel blockers to prevent phencyclidine-induced cognitive dysfunction in the rat: potential for novel treatments for schizophrenia. j pharmacol exp ther, 2011, 338(1): 100-113.
[2]. bagal sk, chapman ml, marron be, et al. recent progress in sodium channel modulators for pain. bioorg med chem lett, 2014, 24(16): 3690-3699.
[3]. zakrzewska jm, palmer j, ettlin da, et al. novel design for a phase iia placebo-controlled, double-blind randomized withdrawal study to evaluate the safety and efficacy of cnv1014802 in patients with trigeminal neuralgia. trials, 2013, 14: 402. |
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| Company Name: |
Moltt Biocem Co., Ltd.
|
| Tel: |
+86-21-38682181 15900741819 |
| Website: |
www.chemicalbook.com/ShowSupplierProductsList15856/0.htm |
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