2349371-81-7
2349371-81-7 structure
- Name: GNE-616
- Chemical Name: GNE-616
- CAS Number: 2349371-81-7
- Molecular Formula: C24H23F4N5O3S
- Molecular Weight: 537.53
- Catalog: Signaling Pathways Membrane Transporter/Ion Channel Sodium Channel
- Create Date: 2019-09-09 13:07:51
- Modify Date: 2024-01-11 01:23:50
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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].
| Name | 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]. |
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| Related Catalog | |
| 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]. |
| References |
| Molecular Formula | C24H23F4N5O3S |
|---|---|
| Molecular Weight | 537.53 |