Size | Price | Stock | Qty |
---|---|---|---|
5mg |
|
||
10mg |
|
||
25mg |
|
||
50mg |
|
||
100mg |
|
||
250mg |
|
||
Other Sizes |
|
Purity: ≥98%
Raxatrigine (also known as GSK-1014802 and CNV-1014802) is a novel, potent small molecule state-dependent sodium channel blocker, the Nav1.7 sodium channel inhibitor. It has the potential to be used as an analgesic and is being developed by Convergence Pharmaceuticals for the treatment of lumbosacral radiculopathy (sciatica) and trigeminal neuralgia (TGN).
ln Vitro |
GSK2 and GSK3 have the same ability to stop PCP-induced reversal learning deficits as lamotrigine, indicating that they may be used to treat cognitive symptoms of schizophrenia. Nonetheless, greater dosages than those needed for the medication's anticonvulsant efficacy are necessary for the reversal learning model to be active, indicating a narrow therapeutic window in comparison to the mechanism-dependent central adverse effects of this indication. The US Food and medicine Administration designated raxatrigine (GSK-1014802) as an orphan medicine in July 2013.
|
---|---|
References |
[1]. Large CH, 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 Jul;338(1):100-13.
|
Molecular Formula |
C18H20CLFN2O2
|
---|---|
Molecular Weight |
350.8150
|
CAS # |
934240-31-0
|
Related CAS # |
Raxatrigine;934240-30-9
|
SMILES |
O=C([C@H]1N[C@@H](C2=CC=C(OCC3=CC=CC=C3F)C=C2)CC1)N.[H]Cl
|
InChi Key |
HEPUBAGOKRIZEO-PPPUBMIESA-N
|
InChi Code |
InChI=1S/C18H19FN2O2.ClH/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)1H/t16-,17+/m1./s1
|
Chemical Name |
(2S,5R)-5-(4-((2-fluorobenzyl)oxy)phenyl)pyrrolidine-2-carboxamide hydrochloride
|
Synonyms |
GSK1014802 GSK 1014802 GSK-1014802 CNV1014802
CNV-1014802 CNV 1014802 Raxatrigine Raxatrigine hydrochloride
Vixotrigine
|
Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
Solubility (In Vitro) |
DMSO : ≥ 31 mg/mL (~88.36 mM)
H2O : ~14.29 mg/mL (~40.73 mM) |
---|---|
Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.13 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.13 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.13 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.8505 mL | 14.2523 mL | 28.5046 mL | |
5 mM | 0.5701 mL | 2.8505 mL | 5.7009 mL | |
10 mM | 0.2850 mL | 1.4252 mL | 2.8505 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.