GSK1014802(CNV1014802)

Novel sodium channel blocker CAS# 934240-30-9

GSK1014802(CNV1014802)

Catalog No. BCC6454----Order now to get a substantial discount!

Product Name & Size Price Stock
GSK1014802(CNV1014802): 5mg $391 In Stock
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Quality Control of GSK1014802(CNV1014802)

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Chemical structure

GSK1014802(CNV1014802)

3D structure

Chemical Properties of GSK1014802(CNV1014802)

Cas No. 934240-30-9 SDF Download SDF
PubChem ID 16046068 Appearance Powder
Formula C18H19FN2O2 M.Wt 314.35
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : 83 mg/mL (264.04 mM; Need ultrasonic and warming)
Chemical Name (2S,5R)-5-[4-[(2-fluorophenyl)methoxy]phenyl]pyrrolidine-2-carboxamide
SMILES C1CC(NC1C2=CC=C(C=C2)OCC3=CC=CC=C3F)C(=O)N
Standard InChIKey JESCETIFNOFKEU-SJORKVTESA-N
Standard InChI InChI=1S/C18H19FN2O2/c19-15-4-2-1-3-13(15)11-23-14-7-5-12(6-8-14)16-9-10-17(21-16)18(20)22/h1-8,16-17,21H,9-11H2,(H2,20,22)/t16-,17+/m1/s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

GSK1014802(CNV1014802) Dilution Calculator

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GSK1014802(CNV1014802) Molarity Calculator

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Preparing Stock Solutions of GSK1014802(CNV1014802)

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 3.1812 mL 15.9058 mL 31.8117 mL 63.6233 mL 79.5292 mL
5 mM 0.6362 mL 3.1812 mL 6.3623 mL 12.7247 mL 15.9058 mL
10 mM 0.3181 mL 1.5906 mL 3.1812 mL 6.3623 mL 7.9529 mL
50 mM 0.0636 mL 0.3181 mL 0.6362 mL 1.2725 mL 1.5906 mL
100 mM 0.0318 mL 0.1591 mL 0.3181 mL 0.6362 mL 0.7953 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

Organizitions Citing Our Products recently

 
 
 

Calcutta University

University of Minnesota

University of Maryland School of Medicine

University of Illinois at Chicago

The Ohio State University

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Yale University

Worcester Polytechnic Institute

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Universidade da Beira Interior

The Institute of Cancer Research

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DRURY University
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Jilin University
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Universite de Paris
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Auckland University
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The University of Tokyo
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Korea University
Korea University

Background on GSK1014802(CNV1014802)

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.

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Description

Raxatrigine (GSK-1014802) is a novel small molecule state-dependent sodium channel blocker; Nav1.7 sodium channel inhibitor.

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