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GX-674

现货
Catalog No.
A8718
Nav1.7拮抗剂
组合的产品项目
规格价格库存 数量
5mg
¥ 3,500.00
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25mg
¥ 12,000.00
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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

StorageStore at -20°C
M.Wt534.95
Cas No.N/A
Formula C21H13ClF2N6O3S2
SolubilitySoluble in DMSO
Chemical Name4-(2-(2-amino-1H-benzo[d]imidazol-5-yl)-4-chlorophenoxy)-2,5-difluoro-N-(1,2,4-thiadiazol-5-yl)benzenesulfonamide
SDFDownload SDF
Canonical SMILESClC1=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
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

质量控制

质量控制和MSDS

批次:

化学结构

GX-674