1. Membrane Transporter/Ion Channel
  2. Sodium Channel
  3. GNE-616

GNE-616 

Cat. No.: HY-126291
Handling Instructions

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.

For research use only. We do not sell to patients.

GNE-616 Chemical Structure

GNE-616 Chemical Structure

CAS No. : 2349371-81-7

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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].

IC50 & Target

Ki: 0.79 nM (hNav1.7)[1]
Kd: 0.38 nM (hNav1.7), 12 nM (hNav1.2), 29 nM (hNav1.6)[1]

In Vitro

Site-directed mutagenesis is critical for the isoform selectivity profile of GNE-616 (hNav1.7, Kd: Y1537s/W1538=170±67 nM, V1541=3.9±1.1 nM, Y1537s/W1538/V1541=790±350 nM)[1].

In Vivo

GNE-616 shows robust activity in a Nav1.7-dependent inherited erythromelalgia (IEM) PK/PD model with an EC50 of 740 nM and EC50,u of 9.6 nM[1].

Molecular Weight

537.53

Formula

C₂₄H₂₃F₄N₅O₃S

CAS No.

2349371-81-7

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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GNE-616
Cat. No.:
HY-126291
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