GSK1014802
- CAS No.
- 934240-30-9
- Chemical Name:
- GSK1014802
- Synonyms
- CS-657;BIIB074);GSK1014802;CNV1014082;Raxatrigine;CNV-1014802;Vixotrigine;MFCD22580419;GSK1014802(CNV1014802);Raxatrigine (GSK1014802)
- CBNumber:
- CB02655408
- Molecular Formula:
- C18H19FN2O2
- Molecular Weight:
- 314.35
- MDL Number:
- MFCD22580419
- MOL File:
- 934240-30-9.mol
- MSDS File:
- SDS
| 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) |
| FDA UNII | QQS4J85K6Y |
| NCI Drug Dictionary | melphalan flufenamide hydrochloride |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS05 |
|---|---|
| Signal word | Danger |
| Hazard statements | H314 |
| Precautionary statements | P260-P280-P303+P361+P353-P304+P340+P310-P305+P351+P338+P310 |
GSK1014802 price More Price(16)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| TRC | R128050 | Raxatrigine | 934240-30-9 | 5mg | $100 | 2021-12-16 | Buy |
| TRC | R128050 | Raxatrigine | 934240-30-9 | 50mg | $710 | 2021-12-16 | Buy |
| ApexBio Technology | B5927 | GSK1014802(CNV1014802) | 934240-30-9 | 50mg | $1339 | 2021-12-16 | Buy |
| ApexBio Technology | B5927 | GSK1014802(CNV1014802) | 934240-30-9 | 100mg | $2126 | 2021-12-16 | Buy |
| American Custom Chemicals Corporation | API0015788 | (2S,5R)-5-(4-([(2-FLUOROPHENYL)METHYL]OXY)PHENYL)-L-PROLINAMIDE 95.00% | 934240-30-9 | 5MG | $504.79 | 2021-12-16 | Buy |
GSK1014802 Chemical Properties,Uses,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
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Hubei Jusheng Technology Co.,Ltd. | 18871490254 | linda@hubeijusheng.com | CHINA | 28180 | 58 |
| BOC Sciences | +1-631-485-4226 | inquiry@bocsci.com | United States | 19553 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6393 | 58 |
| LEAP CHEM CO., LTD. | +86-852-30606658 | market18@leapchem.com | China | 24738 | 58 |
| Wuhan Topule Biopharmaceutical Co., Ltd | +8618327326525 | masar@topule.com | China | 8474 | 58 |
| Zibo Hangyu Biotechnology Development Co., Ltd | +86-0533-2185556 +8617865335152 | Mandy@hangyubiotech.com | China | 11013 | 58 |
| LEAPCHEM CO., LTD. | +86-852-30606658 | market18@leapchem.com | China | 43348 | 58 |
| Amadis Chemical Company Limited | 571-89925085 | sales@amadischem.com | China | 131981 | 58 |
| Shanghai Boyle Chemical Co., Ltd. | sales@boylechem.com | China | 2923 | 55 |