SMILES string
[S](=O)(=O)(Nc4[s]ccn4)c1ccc(cc1)NC(=O)C(c3ccccc3)c2ccccc2
InChI
1S/C23H19N3O3S2/c27-22(21(17-7-3-1-4-8-17)18-9-5-2-6-10-18)25-19-11-13-20(14-12-19)31(28,29)26-23-24-15-16-30-23/h1-16,21H,(H,24,26)(H,25,27)
InChI key
URSQNPPONHUJDL-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 20 mg/mL, clear
storage temp.
room temp
Quality Level
Biochem/physiol Actions
ICA-121431[2,2-二苯基-N-(4-(N-噻唑-2-基氨磺酰基)苯基乙酰胺是一种小分子抑制剂,可靶向VSDIV(域IV电压传感器)中S2和S3中的细胞外氨基酸,这对于Hm1a的功效至关重要。在人体中,ICA-121431可阻断在HEK-293细胞中的上调的TTX敏感的Nav1.3钠通道。
ICA-121431是人Nav1.3和Nav1.1电压门控钠通道的一种有效选择性抑制剂。
ICA-121431是人Nav1.3和Nav1.1电压门控钠通道的有效选择性抑制剂(IC50 = 19 nM),几乎对人Nav1.5或Nav1.7通道没有活性。
signalword
Warning
hcodes
Hazard Classifications
Acute Tox. 4 Oral - Aquatic Chronic 4 - Eye Irrit. 2
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Ken McCormack et al.
Proceedings of the National Academy of Sciences of the United States of America, 110(29), E2724-E2732 (2013-07-03)
Voltage-gated sodium (Nav) channels play a fundamental role in the generation and propagation of electrical impulses in excitable cells. Here we describe two unique structurally related nanomolar potent small molecule Nav channel inhibitors that exhibit up to 1,000-fold selectivity for
Pharmacology of the Nav1. 1 domain IV voltage sensor reveals coupling between inactivation gating processes.
Osteen JD, et al.
Proceedings of the National Academy of Sciences of the USA, 114(26), 6836-6841 (2017)
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