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GNE-131

CAS No. 1629063-81-5

GNE-131( —— )

Catalog No. M23727 CAS No. 1629063-81-5

GNE-131 is a potent and specific inhibitor of human sodium channel NaV1.7 (IC50: 3 nM).

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    GNE-131
  • Note
    Research use only, not for human use.
  • Brief Description
    GNE-131 is a potent and specific inhibitor of human sodium channel NaV1.7 (IC50: 3 nM).
  • Description
    GNE-131 is a potent and specific inhibitor of human sodium channel NaV1.7 (IC50: 3 nM).
  • 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.
  • 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.
  • Synonyms
    ——
  • Pathway
    Membrane Transporter/Ion Channel
  • Target
    Sodium Channel
  • Recptor
    Nav1.7 channel
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    1629063-81-5
  • Formula Weight
    442.57
  • Molecular Formula
    C23H30N4O3S
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO:120 mg/mL (271.14 mM; Need ultrasonic)
  • SMILES
    O=S(C1CC1)(NC2=NN=C3C=C(OCC45CC6CC(C5)CC(C6)C4)C(C7CC7)=CN32)=O
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

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.
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