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GNE-616

CAT: 0804-HY-126291Size: 1 EachDry Ice: NoHazardous: No
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CAT#:0804-HY-126291Size:1 Each
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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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

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