ChemicalBook > CAS DataBase List > GSK1014802

GSK1014802

Product Name
GSK1014802
CAS No.
934240-30-9
Chemical Name
GSK1014802
Synonyms
CS-657;BIIB074);GSK1014802;CNV1014082;CNV-1014802;Vixotrigine;Raxatrigine;MFCD22580419;GSK1014802(CNV1014802);CNV1014802 (GSK-1014802
CBNumber
CB02655408
Molecular Formula
C18H19FN2O2
Formula Weight
314.35
MOL File
934240-30-9.mol
More
Less

GSK1014802 Property

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
More
Less

Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Danger
Hazard statements

H314Causes severe skin burns and eye damage

Precautionary statements

P260Do not breathe dust/fume/gas/mist/vapours/spray.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P303+P361+P353IF ON SKIN (or hair): Remove/Take off Immediately all contaminated clothing. Rinse SKIN with water/shower.

More
Less

N-Bromosuccinimide Price

TRC
Product number
R128050
Product name
Raxatrigine
Packaging
5mg
Price
$100
Updated
2021/12/16
TRC
Product number
R128050
Product name
Raxatrigine
Packaging
50mg
Price
$710
Updated
2021/12/16
ApexBio Technology
Product number
B5927
Product name
GSK1014802(CNV1014802)
Packaging
50mg
Price
$1339
Updated
2021/12/16
ApexBio Technology
Product number
B5927
Product name
GSK1014802(CNV1014802)
Packaging
100mg
Price
$2126
Updated
2021/12/16
American Custom Chemicals Corporation
Product number
API0015788
Product name
(2S,5R)-5-(4-([(2-FLUOROPHENYL)METHYL]OXY)PHENYL)-L-PROLINAMIDE
Purity
95.00%
Packaging
5MG
Price
$504.79
Updated
2021/12/16
More
Less

GSK1014802 Chemical Properties,Usage,Production

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].

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.

GSK1014802 Preparation Products And Raw materials

Raw materials

Preparation Products

More
Less

GSK1014802 Suppliers

Shanghai Boyle Chemical Co., Ltd.
Tel
Fax
86-21-57758967
Email
sales@boylechem.com
Country
China
ProdList
2922
Advantage
55
Chembest Research Laboratories Limited
Tel
+86-21-20908456
Fax
021-58180499
Email
sales@BioChemBest.com
Country
China
ProdList
6005
Advantage
61
Moltt Biocem Co., Ltd.
Tel
+86-21-38682181 15900741819
Fax
+86-21-38682181
Country
China
ProdList
282
Advantage
55
Shanghai Witofly Chemical Co.,Ltd
Tel
Email
sales@witofly.com
Country
China
ProdList
2864
Advantage
52
Jinan Mingya Medical Technology Co., Ltd.
Tel
0531-85828981
Fax
+86-531-85806006
Email
864598798@qq.com
Country
China
ProdList
588
Advantage
58
AdooQ Bioscience CHINA
Tel
025-58849295 18951903616;
Fax
025-68650336
Email
info@adooq.cn
Country
China
ProdList
2990
Advantage
60
LABTER PHARMATECH(BEIJING) CO.,LTD
Tel
010-56330744 18310155299
Fax
010-56330744
Email
sales@labter.com.cn
Country
China
ProdList
23967
Advantage
55
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696,15000506266 15000506266
Fax
+86-21-52996696
Country
China
ProdList
4566
Advantage
55
ShangHai Angti Biotechnology Co., Ltd.
Tel
13764913901
Fax
-
Email
info@angtibio.com
Country
China
ProdList
5004
Advantage
55
Shanghai EFE Biological Technology Co., Ltd.
Tel
021-65675885 18964387627
Fax
021-65675885
Email
info@efebio.com
Country
China
ProdList
9806
Advantage
58

934240-30-9, GSK1014802Related Search:


  • CNV-1014802;RAXATRIGINE;VIXOTRIGINE;BIIB074
  • (5R)-5-{4-[(2-Fluorobenzyl)oxy]phenyl}-L-prolinamide
  • Raxatrigine (GSK1014802)
  • CS-657
  • BIIB074)
  • CNV1014802 (GSK-1014802
  • Vixotrigine
  • GSK1014802
  • CNV-1014802
  • (5R)-5-(4-{[(2-fluorophenyl)methyl]oxy}phenyl)-L-prolinamide
  • GSK1014802(CNV1014802)
  • MFCD22580419
  • (5R)-5-(4-{[(2-fluorophenyl)methyl]oxy}phenyl)-L-prolinamide-HCL
  • (2S,5R)-5-[4-[(2-Fluorophenyl)methoxy]phenyl]-2-pyrrolidinecarboxamide
  • Raxatrigine
  • CNV1014082
  • Melphalan Flufenamide Hydrochloride
  • (R)-5-{4-[(2-Fluorobenzyl)oxy]phenyl}-L-prolinamide
  • CNV1014802;GSK-1014802;GSK-1014802;RAXATRIGINE
  • 2-Pyrrolidinecarboxamide, 5-[4-[(2-fluorophenyl)methoxy]phenyl]-, (2S,5R)-
  • Raxatrigine,Na channels,GSK1014802,Inhibitor,Sodium Channel,GSK 1014802,Na+ channels,inhibit
  • (2S,5R)-5-(4-((2-Fluorobenzyl)oxy)phenyl)pyrrolidine-2-carboxamide
  • 934240-30-9
  • Inhibitors