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[1]

hNav1.7

0.79 nM (Ki)

hNav1.7

0.38 nM (Kd)

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

537.53

Formula

C₂₄H₂₃F₄N₅O₃S

CAS No.
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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
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HY-126291
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