GX-936
Based on 1 Customer Validation
GX-936 (PF-05196233) is a selective Nav1.7 inhibitor. GX-936 binds to the activated VSD4, forms a bidentate salt bridge with the R4 of the S4 helix, traps VSD4 in the activated state, and prevents the channel from recovering from the inactivated state. GX-936 can be used in studies related to pain.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 97.06%
- CAS. Nr.: 1235406-09-3
- Formel: C24H20F3N7O3S2
- Molecular Weight:575.59
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Speicherung:
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
Nav1.7 |
In Vitro
GX-936 binds to the voltage sensor of domain IV in the α-subunit of the NaV1.7 ion channel and forms key interactions to maintain its function as a potent NaV1.7 inhibitor[1].
GX-936 binds to the activated conformation of Nav1.7 VSD4 in a membrane-like environment, locks the voltage sensor domain in this state through interactions with the R4 gating charge and other residues of VSD4, and forms a ternary complex with phosphatidylcholine[2].
GX-936 inhibits Nav1.7 by trapping the VSD4 S4 voltage sensor in an activated state, with its binding mediated by a key salt bridge formed with the S4 R4 residue and selective interactions with VSD4 residues unique to Nav1.7[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 1235406-09-3
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Appearance Solid
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Molecular Weight 575.59
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Formel C24H20F3N7O3S2
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Color White to light yellow
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SMILES
O=S(C1=CC=C(C(C#N)=C1)OC2=CC=C(C=C2C3=CC=NN3C4CN(C4)CC)C(F)(F)F)(NC5=NC=NS5)=O
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Synonyms
PF-05196233
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : ≥ 75 mg/mL (130.30 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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 (protect from light). 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (289 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Storer RI, et al. Highly potent and selective Na1.7 inhibitors for use as intravenous agents and chemical probes. Bioorganic & medicinal chemistry letters. 2017 Nov 01;27(21):4805-4811. [Content Brief]
[2]. 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]
[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]
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 (protect from light). 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 | 1.7373 mL | 8.6867 mL | 17.3735 mL | 43.4337 mL |
| 5 mM | 0.3475 mL | 1.7373 mL | 3.4747 mL | 8.6867 mL | |
| 10 mM | 0.1737 mL | 0.8687 mL | 1.7373 mL | 4.3434 mL | |
| 15 mM | 0.1158 mL | 0.5791 mL | 1.1582 mL | 2.8956 mL | |
| 20 mM | 0.0869 mL | 0.4343 mL | 0.8687 mL | 2.1717 mL | |
| 25 mM | 0.0695 mL | 0.3475 mL | 0.6949 mL | 1.7373 mL | |
| 30 mM | 0.0579 mL | 0.2896 mL | 0.5791 mL | 1.4478 mL | |
| 40 mM | 0.0434 mL | 0.2172 mL | 0.4343 mL | 1.0858 mL | |
| 50 mM | 0.0347 mL | 0.1737 mL | 0.3475 mL | 0.8687 mL | |
| 60 mM | 0.0290 mL | 0.1448 mL | 0.2896 mL | 0.7239 mL | |
| 80 mM | 0.0217 mL | 0.1086 mL | 0.2172 mL | 0.5429 mL | |
| 100 mM | 0.0174 mL | 0.0869 mL | 0.1737 mL | 0.4343 mL |
GX-936 Related Classifications
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