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Chemical Structure : QLS-81
Catalog No.: 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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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.
| M.Wt | 330.40 | |
| Formula | C19H23FN2O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. He-Ling Niu, et al. Acta Pharmacol Sin. 2021 Aug;42(8):1235-1247.
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