VGSC blocker-1

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VGSC blocker-1 

VGSC blocker 1 是 neonatal isoform of the VGSC subtype Nav1.5 (nNav1.5) 的有效小分子阻断剂。VGSC blocker 1 在人乳腺癌细胞系 MDA-MB-231 中,1 μM 处阻断 Ina 峰值电流 34.9%,在 1 μM 处抑制细胞侵袭 0.3%,且不影响细胞活力。

VGSC blocker-1

VGSC blocker-1 Chemical Structure

CAS No. : 2230472-55-4

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生物活性

VGSC blocker-1 is a potent and small molecule blocker of neonatal isoform of the VGSC subtype, Nav1.5 (nNav1.5). VGSC blocker-1 blocks INa peak currents 34.9% at 1 μM and inhibits cell invasion 0.3% at 1 μM in human breast cancer cell line MDA-MB-231, without affecting the cell viability[1].

IC50 & Target

VGSC blocker-1 is a potent and small molecule blocker of neonatal isoform of the VGSC subtype, Nav1.5 (nNav1.5)[1].

体外研究
(In Vitro)

VGSC blocker 1 (compound 1) (1.0 to 10 μM) inhibits human breast cancer cell line MDA-MB-231[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: human breast cancer cell line MDA-MB-231
Concentration: 1.0 to 10μM
Incubation Time: 24 hours
Result: VGSC blocker 1 blocks INa peak currents 34.9% at 1 uMa and inhibits cell invasion 0.3% at 1 uM. These values are much higher than the concentrations required (0.1 μM and 1 μM) to produce significant nNav1.5 current blockade and cell invasion inhibition.

分子量

386.52

Formula

C24H32F2N2

CAS 号

2230472-55-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Dutta S, et al. Discovery and evaluation of nNav1.5 sodium channel blockers with potent cell invasion inhibitory activity in breast cancer cells. Bioorg Med Chem. 2018;26(9):2428-2436.

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