GNE-616
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.
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- No. CAS: 2349371-81-7
- Fòrmula: C24H23F4N5O3S
- Peso molecular:537.53
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Help & FAQs
Actividad biológica
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hNav1.7 0.79 nM (Ki) |
hNav1.7 0.38 nM (Kd) |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 2349371-81-7
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Peso molecular 537.53
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Fòrmula C24H23F4N5O3S
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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
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
GNE-616 Related Classifications
HY-126291 Related Classifications
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