GX-674

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GX-674 is a potent, state-dependent, isoform-selective voltage-gated sodium channel 1.7 (Nav1.7) antagonist with an IC₅₀ of 0.1 nM at -40 mV.

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GX-674 Chemical Structure

CAS No. : 1432913-36-4

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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

GX-674 is a potent, state-dependent, isoform-selective voltage-gated sodium channel 1.7 (Nav1.7) antagonist with an IC₅₀ of 0.1 nM at -40 mV^[1].

IC₅₀ & Target

hNa_v1.7

0.1 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	> 10 μM Compound: 30	Inhibition of human NaV1.5 channel expressed in HEK293 cells by patch clamp electrophysiology assay Inhibition of human NaV1.5 channel expressed in HEK293 cells by patch clamp electrophysiology assay	[PMID: 25927480]
HEK293	IC₅₀	> 10000 nM Compound: 16	Inhibition of full length human Nav1.5 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -60 mV by automated voltage clamp analysis Inhibition of full length human Nav1.5 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -60 mV by automated voltage clamp analysis	[PMID: 26985315]
HEK293	IC₅₀	> 10000 nM Compound: 16	Inhibition of full length human Nav1.4 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 by automated voltage clamp analysis Inhibition of full length human Nav1.4 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 by automated voltage clamp analysis	[PMID: 26985315]
HEK293	IC₅₀	0.2 nM Compound: 16	Inhibition of full length human Nav1.2 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -35 mV by automated voltage clamp analysis Inhibition of full length human Nav1.2 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -35 mV by automated voltage clamp analysis	[PMID: 26985315]
HEK293	IC₅₀	0.3 nM Compound: 16	Inhibition of full length human Nav1.7 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -60 mV by automated voltage clamp analysis Inhibition of full length human Nav1.7 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -60 mV by automated voltage clamp analysis	[PMID: 26985315]
HEK293	IC₅₀	0.3 nM Compound: 16	Inhibition of full length human Nav1.7 channel expressed in HEK cells co-expressing human sodium channel subunit beta3 at -150 mV by manual voltage clamp analysis Inhibition of full length human Nav1.7 channel expressed in HEK cells co-expressing human sodium channel subunit beta3 at -150 mV by manual voltage clamp analysis	[PMID: 26985315]
HEK293	IC₅₀	0.8 nM Compound: 16	Inhibition of full length human Nav1.6 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -35 mV by automated voltage clamp analysis Inhibition of full length human Nav1.6 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -35 mV by automated voltage clamp analysis	[PMID: 26985315]
HEK293	IC₅₀	30 nM Compound: 30	Inhibition of human NaV1.7 channel expressed in HEK293 cells by patch clamp electrophysiology assay Inhibition of human NaV1.7 channel expressed in HEK293 cells by patch clamp electrophysiology assay	[PMID: 25927480]
HEK293	IC₅₀	3850 nM Compound: 16	Inhibition of full length human Nav1.8 channel expressed in HEK cells co-expressing human sodium channel subunit beta3 at holding potential -20 mV by manual voltage clamp analysis Inhibition of full length human Nav1.8 channel expressed in HEK cells co-expressing human sodium channel subunit beta3 at holding potential -20 mV by manual voltage clamp analysis	[PMID: 26985315]
HEK293	IC₅₀	6380 nM Compound: 16	Inhibition of full length human Nav1.1 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -40 mV by automated voltage clamp analysis Inhibition of full length human Nav1.1 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -40 mV by automated voltage clamp analysis	[PMID: 26985315]
HEK293	IC₅₀	9330 nM Compound: 16	Inhibition of full length human Nav1.3 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -50 mV by automated voltage clamp analysis Inhibition of full length human Nav1.3 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -50 mV by automated voltage clamp analysis	[PMID: 26985315]

Molecular Weight

534.95

Formula

C₂₁H₁₃ClF₂N₆O₃S₂

CAS No.

1432913-36-4

SMILES

O=S(C1=CC(F)=C(OC2=CC=C(Cl)C=C2C3=CC=C4N=C(N)NC4=C3)C=C1F)(NC5=NC=NS5)=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]. Ahuja S, et al. Structural basis of Nav1.7 inhibition by an isoform-selective small-molecule antagonist. Science. 2015 Dec 18;350(6267):aac5464. [Content Brief]

GX-674 Related Classifications

Neurological Disease Cardiovascular Disease

Molarity Calculator
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The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass		Concentration		Volume		Molecular Weight *
	=		×		×

The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)	×	Volume _(start)	=	Concentration _(final)	×	Volume _(final)
	×		=		×
C1		V1		C2		V2

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:

GX-6741432913-36-4GX674GX 674Sodium ChannelNa channelsNa+ channelspainneurological disorderscardiovascular disordersstate-dependentInhibitorinhibitorinhibit

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