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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-Sodium Channel-QLS-81
QLS-81

Chemical Structure : QLS-81

CAS No.: 2835455-57-5

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QLS-81 (QLS81)

货号: PC-22308Not For Human Use, Lab Use Only.

QLS-81 is a potent, selective Nav1.7 channel inhibitor with IC50 of 3.5 uM for inhibition of Nav1.7 current in whole-cell patch-clamp recording assay.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

QLS-81 is a potent, selective Nav1.7 channel inhibitor with IC50 of 3.5 uM for inhibition of Nav1.7 current in whole-cell patch-clamp recording assay.
QLS-81 displays 5-fold selectivity over Nav1.4 and Nav1.5 currents.
QLS-81 is 10-fold more potent than its parent compound ralfinamide (IC50=37.1 uM).
QLS-81 (10 μM) caused a hyperpolarizing shift of the fast and slow inactivation of Nav1.7 channel about 7.9 mV and 26.6 mV, respectively, and also slowed down the channel fast and slow inactivation recovery.
QLS-81 (10 μM) inhibited native Nav current and suppressed depolarizing current pulse-elicited neuronal firing in dissociated mouse DRG neurons.
QLS-81 (10 μM) inhibited native Nav current and suppressed depolarizing current pulse-elicited neuronal firing.
QLS-81 (2, 5, 10 mg/kg/day, i.p.) in mice for 10 days dose-dependently alleviated spinal nerve injury-induced neuropathic pain and formalin-induced inflammatory pain.

物理化学性质&存储条件

分子量 330.40
分子式 C19H23FN2O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(S)-2-((3-(4-((2-fluorobenzyl) oxy) phenyl) propyl) amino) propanamide

参考文献

1. He-Ling Niu, et al. Acta Pharmacol Sin. 2021 Aug;42(8):1235-1247.

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