GSK1014802(CNV1014802) (Synonyms: GSK-1014802; CNV1014802) |
| Catalog No.GC10234 |
GSK1014802(CNV1014802) (GSK-1014802) est un nouveau bloqueur de canal sodique dépendant de l'état de la petite molécule ; Inhibiteur du canal sodique Nav1.7.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 934240-30-9
Sample solution is provided at 25 µL, 10mM.
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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.
| Cas No. | 934240-30-9 | SDF | |
| Synonymes | GSK-1014802; CNV1014802 | ||
| Chemical Name | (2S,5R)-5-(4-((2-fluorobenzyl)oxy)phenyl)pyrrolidine-2-carbimidic acid | ||
| Canonical SMILES | FC1=CC=CC=C1COC2=CC=C([C@@](N3)([H])CC[C@@]3([H])C(O)=N)C=C2 | ||
| Formula | C18H19FN2O2 | M.Wt | 314.35 |
| Solubility | DMSO : 83 mg/mL (264.04 mM; Need ultrasonic and warming) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.1812 mL | 15.9058 mL | 31.8117 mL |
| 5 mM | 0.6362 mL | 3.1812 mL | 6.3623 mL |
| 10 mM | 0.3181 mL | 1.5906 mL | 3.1812 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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