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GX-674 Nav1.7 antagonist

Catalog No.A8718
Size Price Stock
5mg
$350.00
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25mg
$1,200.00
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Sample solution is provided at 25 µL, 10mM.

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Quality Control & MSDS

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Chemical structure

GX-674

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Chemical Properties

Cas No. N/A SDF Download SDF
Synonyms N/A
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
Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

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.