GNE-616

• Description :

  GNE-616 is a highly potent, metabolically stable, orally bioavailable, and subtype selective Nav1.7 inhibitor (Ki of 0.79 nM and Kd of 0.38 nM for hNav1.7) for the treatment of chronic pain. GNE-616 shows >1000 nM Kd and >2500-fold selectivity over hNav1.1, hNav1.3, hNav1.4, and hNav1.5. Selectivity over hNav1.2 and hNav1.6 is more modest at 31- and 73-fold, respectively[1].

• CAS Number :

  [2349371-81-7]

• UNSPSC :

  12352005

• Target :

  Sodium Channel

• Type :

  Reference compound

• Related Pathways :

  Membrane Transporter/Ion Channel

• Applications :

  Neuroscience-Neuromodulation

• Field of Research :

  Neurological Disease

• Assay Protocol :

  https://www.medchemexpress.com/gne-616.html

• Solubility :

  10 mM in DMSO

• Smiles :

  O=S(C1=C(F)C=C2[C@@H](N3[C@@H](C4=NC=CC=C4)C[C@@H](C(F)(F)F)CC3)CCOC2=C1)(NC5=NC=NC=C5)=O

• Molecular Formula :

  C24H23F4N5O3S

• Molecular Weight :

  537.53

• References & Citations :

  [1]McKerrall SJ, et al. Structure- and Ligand-Based Discovery of Chromane Arylsulfonamide Nav1.7 Inhibitors for the Treatment of Chronic Pain. J Med Chem. 2019 Apr 25;62 (8) :4091-4109.

• Shipping Conditions :

  Room temperature

• Scientific Category :

  Reference compound1

• Clinical Information :

  No Development Reported

• Isoform :

  Nav1.7