GX-674
Based on 1 Customer Validation
GX-674 is a selective NaV1.7 inhibitor with an IC50 of 0.1 nM against hNaV1.7. GX-674 can be used for research on pain, neuropathic pain, and arrhythmia.
For research use only. We do not sell to patients.
- Purity : 98.45%
- CAS No.: 1432913-36-4
- Formula: C21H13ClF2N6O3S2
- Molecular Weight:534.95
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
IC50 & Target
[1]|
hNav1.7 0.1 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
>10 μM
Compound: 30
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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
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[PMID: 25927480] |
| HEK293 | IC50 |
30 nM
Compound: 30
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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
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[PMID: 25927480] |
| HEK293 | IC50 |
>10000 nM
Compound: 16
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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
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[PMID: 26985315] |
| HEK293 | IC50 |
0.2 nM
Compound: 16
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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
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[PMID: 26985315] |
| HEK293 | IC50 |
0.3 nM
Compound: 16
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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
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[PMID: 26985315] |
| HEK293 | IC50 |
0.3 nM
Compound: 16
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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
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[PMID: 26985315] |
| HEK293 | IC50 |
0.8 nM
Compound: 16
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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
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[PMID: 26985315] |
| HEK293 | IC50 |
3850 nM
Compound: 16
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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
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[PMID: 26985315] |
| HEK293 | IC50 |
6380 nM
Compound: 16
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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
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[PMID: 26985315] |
| HEK293 | IC50 |
9330 nM
Compound: 16
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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
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[PMID: 26985315] |
| HEK293 | IC50 |
>10000 nM
Compound: 16
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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
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[PMID: 26985315] |
In Vitro
GX-674 binds to the extracellular part of VSD-IV on NaV1.7, interacting with the fourth positively charged arginine residue (R1608) on VSD-IV-S4[1].
GX-674 exhibits a fast association rate for blocking hNaV1.7, similar to that of TTX[2].
GX-674 is a highly potent and state-dependent inhibitor of human Nav1.7 that binds to the activated state of the VSD4 voltage-sensor, forming a critical salt-bridge interaction with the R4 residue, which is essential for its high potency[3].
GX-674 exhibits exceptionally high selectivity for human NaV1.7 over NaV1.5 (approximately 100,000-fold) and its activity is critically dependent on the R1608 residue[4].
GX-674 enables the pharmacological isolation of non-NaV1.5 sodium currents in NaV1.5GX/GX adult mouse ventricular myocytes, revealing that NaV1.8 and NaV1.4 contribute significantly to INa in healthy cardiomyocytes[5].
Physiological characterization of GX-674 on hNaV1.7 VSD IV reveals that the R4 gating charge on S4 and the YWxxV motif on S2 are critical determinants for compound potency and selectivity[7].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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CAS No. 1432913-36-4
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Appearance Solid
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Molecular Weight 534.95
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Formula C21H13ClF2N6O3S2
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Color Off-white to light brown
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Cardiac voltage-sensitive optical mapping
Cardiac voltage-sensitive optical mapping records changes in transmembrane potential from cardiac tissue by staining the preparation with a voltage-sensitive dye and imaging fluorescence changes during electrical activation; the resulting optical action potentials can be used to map activation time, action potential duration, conduction velocity, wavefront propagation, and arrhythmia dynamics. The optical signal represents a relative fluorescence change from a tissue volume rather than a single-cell intracellular recording, so spatial resolution, sampling rate, voltage resolution, optical magnification, light penetration, and motion control must be considered together when interpreting optical action potentials.
Purity & Documentation
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Data Sheet (279 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Goodchild SJ, et al. Molecular Pharmacology of Selective Na1.6 and Dual Na1.6/Na1.2 Channel Inhibitors that Suppress Excitatory Neuronal Activity Ex Vivo. ACS chemical neuroscience. 2024 Mar 20;15(6):1169-1184. [Content Brief]
[2]. Bankar G, et al. Selective Na1.7 Antagonists with Long Residence Time Show Improved Efficacy against Inflammatory and Neuropathic Pain. Cell reports. 2018 Sep 18;24(12):3133-3145. [Content Brief]
[3]. Payandeh J, et al. Selective Ligands and Drug Discovery Targeting the Voltage-Gated Sodium Channel Nav1.7. Handbook of experimental pharmacology. 2018;246:271-306. [Content Brief]
[5]. Clark CJ. Sodium Current Composition and Remodeling in Murine Cardiomyocytes (Doctoral dissertation.
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 |
GX-674 Related Classifications
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