GX 201

Key Product Details

Product Description

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.

Product Specifications for GX 201

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Preparing Stock Solutions for GX 201

The following data is based on the product molecular weight 563.00.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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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

Calculators

Background References

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

Product Documents for GX 201