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
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
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.
N-Bromosuccinimide Price
- Product number
- R128050
- Product name
- Raxatrigine
- Packaging
- 5mg
- Price
- $100
- Updated
- 2021/12/16
- Product number
- R128050
- Product name
- Raxatrigine
- Packaging
- 50mg
- Price
- $710
- Updated
- 2021/12/16
- Product number
- B5927
- Product name
- GSK1014802(CNV1014802)
- Packaging
- 2mg
- Price
- $158
- Updated
- 2021/12/16
- Product number
- CS-4038
- Product name
- Raxatrigine
- Purity
- 99.47%
- Packaging
- 5mg
- Price
- $180
- Updated
- 2021/12/16
- Product number
- B5927
- Product name
- GSK1014802(CNV1014802)
- Packaging
- 5mg
- Price
- $236
- Updated
- 2021/12/16
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].
Synthesis
934240-62-7
934240-30-9
Methyl (2S,5R)-5-(4-((2-fluorobenzyl)oxy)phenyl)pyrrolidine-2-carboxylate (6.4 g, 19.43 mmol) was used as a raw material, which was mixed with a methanol solution of 7 M ammonia (52.47 mL, 367.27 mmol) in a sealed flask and stirred. The reaction mixture was allowed to stand at room temperature for 4 days before the solvent was removed by rotary evaporation. Toluene (12 mL) was then added and evaporated again to remove residual methanol. The solid obtained was suspended in toluene (10.5 mL) and stirred for 2 h. Heptane (3.5 mL) was then added and stirring was continued at room temperature for 30 min, followed by cooling in an ice bath and stirring for 30 min. The solid was collected by filtration, washed first with cold 3:1 toluene/heptane solvent mixture (12 mL), then with heptane (12 mL), and blotted dry. The solid was dried in a vacuum oven at 45 °C to give a beige solid product (5.85 g).NMR analysis showed the presence of trace impurities in the aromatic region (6.8-6.9 ppm), which were presumed to be possibly unreacted phenol. For this purpose, the product was dissolved in ethyl acetate (200 mL), washed sequentially with 2% Na2CO3 solution (2 × 100 mL) and water (100 mL), and the organic phase was dried with Na2SO4 and concentrated to give an off-white powdery product (5.47 g, 90% yield).LC-MS analysis showed MH+ = 315 (corresponding to molecular formula C18H19FN2O2) NMR (CDCl3) data were as follows: δ 1.68 (1H, m), 2.06-2.35 (3H, m), 2.51 (1H, br s), 3.88 (1H, dd, J = 3Hz, 9Hz), 4.31 (1H, dd, J = 6Hz, 9Hz), 5.15 (2H, s), 5.57 (1H, br s), 6.99 ( 2H, d, J = 9Hz), 7.11 (1H, m), 7.18 (1H, m), 7.30-7.40 (3H, m), 7.53 (1H, m).
IC 50
Nav1.7
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
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