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GX-674 Sale

目录号 : GC16545

GX-674 是一种有效的、状态依赖性、异构体选择性电压门控钠通道 1.7 (Nav1.7) 拮抗剂,在 -40 mV 时的 IC50 为 0.1 nM。

GX-674 Chemical Structure

Cas No.:1432913-36-4

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5mg
¥2,405.00
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25mg
¥8,411.00
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Sample solution is provided at 25 µL, 10mM.

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产品描述

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
化学名 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
分子式 C21H13ClF2N6O3S2 分子量 534.95
溶解度 Soluble in DMSO 储存条件 Store at -20°C
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溶解性数据

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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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