1. Membrane Transporter/Ion Channel
  2. Sodium Channel
  3. GX-674

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.

For research use only. We do not sell to patients.

GX-674

GX-674 Chemical Structure

CAS No. : 1432913-36-4

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Customer Review

Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

  • References

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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

hNav1.7

0.1 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
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]
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 Nav1.4 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
> 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]
Molecular Weight

534.95

Formula

C21H13ClF2N6O3S2

CAS No.
Appearance

Solid

Color

Off-white to light brown

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
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (93.47 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8693 mL 9.3467 mL 18.6933 mL
5 mM 0.3739 mL 1.8693 mL 3.7387 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 98.45%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8693 mL 9.3467 mL 18.6933 mL 46.7333 mL
5 mM 0.3739 mL 1.8693 mL 3.7387 mL 9.3467 mL
10 mM 0.1869 mL 0.9347 mL 1.8693 mL 4.6733 mL
15 mM 0.1246 mL 0.6231 mL 1.2462 mL 3.1156 mL
20 mM 0.0935 mL 0.4673 mL 0.9347 mL 2.3367 mL
25 mM 0.0748 mL 0.3739 mL 0.7477 mL 1.8693 mL
30 mM 0.0623 mL 0.3116 mL 0.6231 mL 1.5578 mL
40 mM 0.0467 mL 0.2337 mL 0.4673 mL 1.1683 mL
50 mM 0.0374 mL 0.1869 mL 0.3739 mL 0.9347 mL
60 mM 0.0312 mL 0.1558 mL 0.3116 mL 0.7789 mL
80 mM 0.0234 mL 0.1168 mL 0.2337 mL 0.5842 mL
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  • 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.

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Product Name:
GX-674
Cat. No.:
HY-123825
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