GX-674 |
| Catalog No.GC16545 |
Nav1.7 antagonist
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1432913-36-4
Sample solution is provided at 25 µL, 10mM.
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GX-674 is an aryl sulfonamide class of antagonists that inhibits Nav1.7 [1]
Nav (voltage-gated sodium) channels conduct ionic currents that initiate action potentials in neurons and muscles cells. Human express 9 Nav channel isoforms (Nav 1.1-1.9), among which Nav 1.7 channel are express in olfactory epithelium, sympathetic ganglion, and dorsal root ganglion sensory neurons. Gain-of-function mutations in Nav1.7 are associated with extreme pain disorders whereas loss-of-function mutations cause congenital insensitivity to pain in individuals. [1]
In HEK293 cells, patch clamp analysis was perform for human Nav channels. GX-674 shows potent inhibition effect on Nav.1.7 (IC50= 0.1nM). GX-674 also exhibits substantial selectivity on different Nav subtypes. It shows much higher inhibitory effects on Nav 1.7 over other Nav isoform, such as 100000 times more potent for Nav1.7 than for Nav 1.5. GX-74 is also reported to bind to a high-affinity, isoform-selective, and extracellularly accessible site on VSD4. (i.e. one of the peripheral voltage-sensor domains of Nav.1.7). [1]
Reference:
1. Ahuja S, Mukund S, Deng L et al. Structural basis of Nav1.7 inhibition by an isoform-selective small-molecule antagonist. Science. 2015 Dec 18;350(6267):aac5464.
| Cas No. | 1432913-36-4 | SDF | |
| Chemical Name | 4-(2-(2-amino-1H-benzo[d]imidazol-5-yl)-4-chlorophenoxy)-2,5-difluoro-N-(1,2,4-thiadiazol-5-yl)benzenesulfonamide | ||
| Canonical SMILES | ClC1=CC(C2=CC(N=C(N)N3)=C3C=C2)=C(OC4=C(F)C=C(S(NC5=NC=NS5)(=O)=O)C(F)=C4)C=C1 | ||
| Formula | C21H13ClF2N6O3S2 | M.Wt | 534.95 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 |
| 10 mM | 0.1869 mL | 0.9347 mL | 1.8693 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 1 reference(s) in Google Scholar.)
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