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1629063-81-5

1629063-81-5 structure
1629063-81-5 structure
  • Name: GNE-131
  • Chemical Name: GNE-131
  • CAS Number: 1629063-81-5
  • Molecular Formula: C23H30N4O3S
  • Molecular Weight: 442.57
  • Catalog: Signaling Pathways Membrane Transporter/Ion Channel Sodium Channel
  • Create Date: 2019-01-20 17:59:14
  • Modify Date: 2024-03-03 13:07:16
  • GNE-131 is a potent and selective inhibitor of human sodium channel NaV1.7, with an IC50 of 3 nM.

Name GNE-131
Description GNE-131 is a potent and selective inhibitor of human sodium channel NaV1.7, with an IC50 of 3 nM.
Related Catalog
Target

IC50: 3 nM (hNaV1.7)[1].

In Vitro GNE-131 (Compound 13) shows moderate clearance in human liver microsomes and excellent functional activity against human NaV1.7 with an IC50 of 0.003±0.001 μM. GNE-131 shows excellent potency, good in vitro metabolic stability[1].
In Vivo GNE-131 shows low in vivo clearance in mouse, rat, and dog. GNE-131 also displays excellent efficacy in a transgenic mouse model of induced pain[1].
References

[1]. Focken T, et al. Design of Conformationally Constrained Acyl Sulfonamide Isosteres: Identification of N-([1,2,4]Triazolo[4,3- a]pyridin-3-yl)methane-sulfonamides as Potent and Selective hNaV1.7 Inhibitors for the Treatment of Pain. J Med Chem. 2018 Jun 14;61(11):4810-4831.

Molecular Formula C23H30N4O3S
Molecular Weight 442.57
Storage condition 2-8℃
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