An inhibitor of Nav1.7
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GNE-131

Item No. 45386

Product Insert (PDF)
Technical Information
Formal Name
N-[6-cyclopropyl-7-(tricyclo[3.3.1.13,7]dec-1-ylmethoxy)-1,2,4-triazolo[4,3-a]pyridin-3-yl]-cyclopropanesulfonamide
CAS Number
1629063-81-5
Molecular Formula
C23H30N4O3S
Formula Weight
442.6
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥10 mg/ml
SMILES
O=[S](NC1=NN=C2C=C(C(C3CC3)=CN21)OCC4(C[C@@H](C5)C6)C[C@@H]6C[C@@H]5C4)(C7CC7)=O
InChi Code
InChI=1S/C23H30N4O3S/c28-31(29,18-3-4-18)26-22-25-24-21-8-20(19(12-27(21)22)17-1-2-17)30-13-23-9-14-5-15(10-23)7-16(6-14)11-23/h8,12,14-18H,1-7,9-11,13H2,(H,25,26)/t14-,15+,16-,23?
InChi Key
FPERPEQIXLOVIK-QUXYOMGYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $65

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    5 mg

    $293

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    10 mg

    $488

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    25 mg

    $975

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    Product Description

    GNE-131 is an inhibitor of voltage-gated sodium channel 1.7 (Nav1.7; IC50 = 0.003 µM).1 It is selective for Nav1.7 over Nav1.1, Nav1.2, Nav1.5, and Nav1.6 (IC50s = 0.045, 0.007, 0.110, and 0.092 µM, respectively). In vivo, GNE-131 (30 mg/kg) reduces aconitine-induced nocifensive behavior in a transgenic mouse model of inherited erythromelalgia (IEM).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Focken, T., Chowdhury, S., Zenova, A., 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. 61(11), 4810-4831 (2018).