CNV1014802

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

CNV1014802 (GSK-1014802, Raxatrigine, Vixotrigine, BIIB074) 是一种有效的选择性 Nav1.7 钠通道阻滞剂。

CNV1014802 (GSK-1014802, Raxatrigine, Vixotrigine, BIIB074) is a potent, selective Nav1.7 sodium channel blocker, shows analgesic effects and potential in the treatment of cognitive symptoms of schizophrenia in vivo.Pain Phase 2 Clinical(In Vitro):Like lamotrigine, both GSK2 and GSK3 were able to prevent the deficit in reversal learning produced by PCP, thus confirming their potential in the treatment of cognitive symptoms of schizophrenia. However, higher doses than those required for anticonvulsant efficacy of the drugs were needed for activity in the reversal-learning model, suggesting a lower therapeutic window relative to mechanism-dependent central side effects for this indication. Raxatrigine (GSK-1014802) received orphan-drug designation from the US Food and Drug Administration in July 2013.

Like lamotrigine, both GSK2 and GSK3 were able to prevent the deficit in reversal learning produced by PCP, thus confirming their potential in the treatment of cognitive symptoms of schizophrenia. However, higher doses than those required for anticonvulsant efficacy of the drugs were needed for activity in the reversal-learning model, suggesting a lower therapeutic window relative to mechanism-dependent central side effects for this indication. Raxatrigine (GSK-1014802) received orphan-drug designation from the US Food and Drug Administration.

——

GSK-1014802 | CNV-1014802 | Raxatrigine | Vixotrigine | BIIB074

Membrane Transporter/Ion Channel

Sodium Channel

SodiumChannel

Neurological Disease

Pain

934240-30-9

314.3541

C18H19FN2O2

>98% (HPLC)

10 mM in DMSO

C1CC(NC1C2=CC=C(C=C2)OCC3=CC=CC=C3F)C(=O)N

2-Pyrrolidinecarboxamide, 5-[4-[(2-fluorophenyl)methoxy]phenyl]-, (2S,5R)-

(-20℃)

With Ice Pack

≥ 2 years