GNE-616

Cat. No.: HY-126291: FAQs
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GNE-616 is a highly potent, metabolically stable, orally bioavailable, and subtype selective Nav1.7 inhibitor (K_i of 0.79 nM and K_d of 0.38 nM for hNav1.7) for the treatment of chronic pain. GNE-616 shows >1000 nM K_d 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

CAS No. : 2349371-81-7

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•Related Small Molecules:

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View All Isoforms

Na_v1.1 Na_v1.2 Na_v1.3 Na_v1.4 Na_v1.5 Na_v1.6 Na_v1.7 Na_v1.8

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

hNa_v1.7

0.79 nM (Ki)

hNa_v1.7

0.38 nM (Kd)

In Vitro

Site-directed mutagenesis is critical for the isoform selectivity profile of GNE-616 (hNav1.7, K_d: 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.

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].

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

Molecular Weight

537.53

Formula

C₂₄H₂₃F₄N₅O₃S

CAS No.

2349371-81-7

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[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. [Content Brief]

GNE-616 Related Classifications

Neurological Disease

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GNE-6162349371-81-7GNE616GNE 616Sodium ChannelNa channelsNa+ channelsInhibitorinhibitorinhibit

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