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Submit ReviewGX 201
Description: Potent and selective Nav1.7 blocker; analgesic
Chemical Name: 4-[[1-[[2-Chloro-5-(trifluoromethyl)phenyl]methyl]-4-piperidinyl]methoxy]-5-cyclopropyl-2-fluoro-N-(methylsulfonyl)benzamide
Purity: ≥98% (HPLC)
Biological Activity for GX 201
GX 201 is a potent and selective Nav1.7 blocker (IC50 = 3.2 nM). Exhibits 10x selectivity for Nav1.7 over Nav1.1, Nav1.2, and Nav1.6 channels. Displays prolonged residency time on the Nav1.7 channel. Chronic dosing increases compound potency ~10-fold and provides efficacy that persists after the compound has cleared from plasma. Suppresses neuropathic pain in a mouse diabetic neuropathy model. Analgesic.
Compound Libraries for GX 201
GX 201 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for GX 201
| M. Wt | 563 |
| Formula | C25H27ClF4N2O4S |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1788071-27-1 |
| PubChem ID | 118120545 |
| InChI Key | KYBPOTYVFWNSGS-UHFFFAOYSA-N |
| Smiles | CS(=O)(NC(C1=CC(C2CC2)=C(C=C1F)OCC3CCN(CC3)CC4=CC(C(F)(F)F)=CC=C4Cl)=O)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for GX 201
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 56.3 | 100 |
Preparing Stock Solutions for GX 201
The following data is based on the product molecular weight 563. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.78 mL | 8.88 mL | 17.76 mL |
| 5 mM | 0.36 mL | 1.78 mL | 3.55 mL |
| 10 mM | 0.18 mL | 0.89 mL | 1.78 mL |
| 50 mM | 0.04 mL | 0.18 mL | 0.36 mL |
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Product Datasheets for GX 201
References for GX 201
References are publications that support the biological activity of the product.
Shields et al (2018) Insensitivity to pain upon adult-onset deletion of NaV1.7 or its blockade with selective inhibitors J.Neurosci. 38 10180 PMID: 30301756
Banker et al (2018) Selective NaV1.7 antagonists with long residence time show improved efficacy against inflammatory and neuropathic pain. Cell Rep. 24 3133 PMID: 30231997
If you know of a relevant reference for GX 201, please let us know.
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Keywords: GX 201, GX 201 supplier, GX201, Potent, selective, Nav1.7, voltage-gated, Sodium, NaV, Channels, blockers, blocks, inhibitors, inhibits, neuropathic, pain, slow, dissociation, Voltage-gated, 7029, Tocris Bioscience
Citations for GX 201
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