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GX-674

Catalog No.GC16545

Nav1.7 antagonist

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GX-674 Chemical Structure

Cas No.: 1432913-36-4

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5mg
$236.00
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25mg
$825.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

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.

Chemical Properties

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.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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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
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