GX 201

Name: GX 201
Brand: Tocris Bioscience
SKU: 7029

Tocris Bioscience, part of Bio-Techne | Catalog # 7029

COA / SDS

Potent and selective Nav1.7 blocker; analgesic

Key Product Details

Description:	Potent and selective Na_v1.7 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)
Molecular Weight:	563

View Full Technical Details for GX 201

Technical Data
Citations

Biological Activity for GX 201

GX 201 is a potent and selective Na_v1.7 blocker (IC₅₀ = 3.2 nM). Exhibits 10x selectivity for Na_v1.7 over Na_v1.1, Na_v1.2, and Na_v1.6 channels. Displays prolonged residency time on the Na_v1.7 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 for GX 201

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
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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References for GX 201

References are publications that support the biological activity of the product.

Banker Selective Na_V1.7 antagonists with long residence time show improved efficacy against inflammatory and neuropathic pain. Cell Rep. 2018 PMID: 30231997
Shields Insensitivity to pain upon adult-onset deletion of Na_V1.7 or its blockade with selective inhibitors J.Neurosci. 2018 PMID: 30301756