GSK1014802(CNV1014802)Novel sodium channel blocker CAS# 934240-30-9 |
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Quality Control & MSDS
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| 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. |
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| 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. |
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| 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
GSK1014802(CNV1014802) Molarity Calculator
| 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. | |||||
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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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