GX 201

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Cat.No. 7029 - GX 201 | C25H27ClF4N2O4S | CAS No. 1788071-27-1
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)
Datasheet
Citations
Reviews
Literature (5)

Biological Activity

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.

Technical Data

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

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 56.3 100

Preparing Stock Solutions

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.

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

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


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Citations for GX 201

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