GX-936 | Nav1.7 Inhibitor | CAS# 1235406-09-3 - InvivoChem
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GX-936
GX-936 Chemical Structure CAS No.: 1235406-09-3 Product category: New1 This product is for research use only, not for human use. We do not sell to patients. | Size | Price |
|---|---|
| 500mg | |
| 1g | |
| Other Sizes |
- Business Relationship with 5000+ Clients Globally
- Major Universities, Research Institutions, Biotech & Pharma
- Citations by Top Journals: Nature, Cell, Science, etc.
Nature 2025, 643(8070):192-200.
Nature 2024 Dec 18.
Nature 2021, 597(7874):119-125.
Cell 2020,183:1202-1218.e25.
Science Adv 2022: 8, eabm9427.
Nat Neurosci 2024, 27:1468-1474.
Science Adv 2025, 11(33):eadr5199.
Nat Metab 2024, 6: 1108-1127.
Cell Stem Cell 2024, 31:106-126.e13.
Nature 597, 119–125 (2021)
Cell Stem Cell 2020,26(6):845-861.e12.
Science Trans Med 2023,15(701):eadd7872.
STTT 2023,8(1):91.
Cell Reports 2023,42(4):112313
Science Trans Med 2023, 15: eadd7872.
Cancer Cell 2021,39(4):529-547.e7.
Cancer Discov 2022,12(4):1106-1127.
Immunity 2024,57:2651-2668.e12.
Immunity 2023,56(3):620-634.e11.
J Am Chem Soc 2022,144:21831-21836.
Cell 2020,183:1202-1218.e25.
Science Adv 2022:8,eabm9427.
Nature 2021,597(7874):119-125.
Cell 2020,183:1202-1218.e25.
PNAS Nexus 2022,1(3):pgac063.
ACS Nano 2023,17(10):9110-9125.
Biomaterial 2023 Sep16:302:122333. - Product Description
- Bioactivity & Protocols
- Physicochemical Properties
- Solubility Data
- Calculators
GX-936 (GX936; PF-05196233; PF 05196233) is a novel and potent Nav1.7 inhibitor with the potential to be used to treat cardiovascular and neurological disorders. It acts by binding to the activated state of voltage-sensor domain IV (VSD4), and shows robust inhibition of the 1KαPMTX-evoked N1742K response (IC50 =40 nM). Voltage-gated sodium (Nav) channels propagate action potentials in excitable cells. Accordingly, Nav channels are therapeutic targets for many cardiovascular and neurological disorders.
Biological Activity I Assay Protocols (From Reference)| References | Science. 2015 Dec 18;350(6267):aac5464. doi: 10.1126/science.aac5464. |
|---|
| Molecular Formula | C24H20F3N7O3S2 |
|---|---|
| Molecular Weight | 575.585911750793 |
| Exact Mass | 575.102 |
| CAS # | 1235406-09-3 |
| PubChem CID | 46841936 |
| Appearance | Typically exists as solid at room temperature |
| LogP | 3.9 |
| Hydrogen Bond Donor Count | 1 |
| Hydrogen Bond Acceptor Count | 13 |
| Rotatable Bond Count | 8 |
| Heavy Atom Count | 39 |
| Complexity | 1000 |
| Defined Atom Stereocenter Count | 0 |
| InChi Key | UCAVSLIXTXZSRD-UHFFFAOYSA-N |
| InChi Code | InChI=1S/C24H20F3N7O3S2/c1-2-33-12-17(13-33)34-20(7-8-30-34)19-10-16(24(25,26)27)3-5-22(19)37-21-6-4-18(9-15(21)11-28)39(35,36)32-23-29-14-31-38-23/h3-10,14,17H,2,12-13H2,1H3,(H,29,31,32) |
| Chemical Name | 3-Cyano-4-[2-[1-(1-ethyl-3-azetidinyl)-1H-pyrazol-5-yl]-4-(trifluoromethyl)phenoxy]-N-1,2,4-thiadiazol-5-yl-benzenesulfonamide |
| Synonyms | GX936 GX 936 GX-936PF05196233 PF 05196233 PF-05196233 |
| HS Tariff Code | 2934.99.9001 |
| Storage | Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition | Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs) |
| Solubility (In Vitro) | May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples |
|---|---|
| Solubility (In Vivo) | Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples. Injection Formulations (e.g. IP/IV/IM/SC) Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] *Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline) Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline) Injection Formulation 7: Ethanol : Cremophor : Saline = 10: 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline) Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil) Injection Formulation 10: EtOH : PEG300:Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Oral Formulations Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View MoreOral Formulation 3: Dissolved in PEG400 Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose Oral Formulation 6: Mixing with food powders Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.  (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg |
| 1 mM | 1.7373 mL | 8.6867 mL | 17.3735 mL |
| 5 mM | 0.3475 mL | 1.7373 mL | 3.4747 mL |
| 10 mM | 0.1737 mL | 0.8687 mL | 1.7373 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
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Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
Note: (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving. (2) Be sure to add the solvent(s) in order.
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