QX 314 chloride

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QX 314 chloride

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

5369-03-9

包装与价格：

包装	价格(元)
10mM (in 1mL DMSO)	电议
50mg	电议

产品介绍

化学性质

Physical Appearance	A solid
Storage	Store at RT
M.Wt	298.85
Cas No.	5369-03-9
Formula	C₁₆H₂₇N₂OCl
Solubility	insoluble in EtOH; ≥14.95 mg/mL in DMSO with gentle warming; ≥22.3 mg/mL in H2O
Chemical Name	2-((2,6-dimethylphenyl)amino)-N,N,N-triethyl-2-oxoethanaminium chloride
Canonical SMILES	O=C(C[N+](CC)(CC)CC)NC1=C(C)C=CC=C1C.[Cl-]
运输条件	蓝冰运输或根据您的需求运输。
一般建议	为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。

资料参考

QX 314 chloride is a relatively membrane-impermeable lidocaine derivative that selectively blocks voltage-activated Na⁺channels on nociceptive neurons and induces a preferential nociceptive block, presumably by permeating through the channel pore of the capsaicin receptor transient receptor potential vanilloid 1 (TRPV1), as well as the pore of transient receptor potential cation channel, subfamily A, member 1 (TRPA1). When applied externally, QX 314 chloride alone exhibits no effect on the activity of Na⁺channels in small sensory neurons, but when applied in the presence of the TRPV1 agonist capsaicin, QX 314 chloride blocks sodium channels and inhibits sensory neuron excitability. In addition, QX 314 chloride is also effective on motor neurons, capable of inducing a strong and long-lasting motor block.

References:

1. Stueber T, Eberhardt MJ, Hadamitzky C, et al. Quaternary Lidocaine Derivative QX-314 Activates and Permeates Human TRPV1 and TRPA1 to Produce Inhibition of Sodium Channels and Cytotoxicity. Anesthesiology, 2016, 124(5): 1153-1165.

2. Binshtok AM, Bean BP, Woolf CJ. Inhibition of nociceptors by TRPV1-mediated entry of impermeant sodium channel blockers. Nature, 2007, 449(7162): 607-610.

试验操作

Cell experiment:[1]
Cell lines	Human embryonic kidney 293 (HEK-293) cells expressing hTRPV1 or hTRPA1, as well as the sodium channel Nav1.7
Reaction Conditions	5 mM QX 314 chloride
Applications	Coapplication of 5 mM QX 314 chloride and capsaicin (for activation of hTRPV1) resulted in a prominent use-dependent inhibition of sodium currents. Similarly, 5 mM QX 314 chloride in combination with 200 μM carvacrol (for activation of hTRPA1) produced a significantly stronger use-dependent block of sodium currents in cells expressing hTRPA1 compared with carvacrol alone.
Animal experiment:[2]
Animal models	Sprague-Dawley rats
Dosage form	0.2%, 100 ml Regional injection
Applications	Injection of QX 314 chloride together with capsaicin into rat hindpaws produced a long-lasting (more than 2 h) increase in mechanical and thermal nociceptive thresholds. Long-lasting decreases in pain sensitivity were also seen with regional injection of QX 314 chloride and capsaicin near the sciatic nerve.
Note	The technical data provided above is for reference only.
	References: 1. Stueber T, Eberhardt MJ, Hadamitzky C, et al. Quaternary Lidocaine Derivative QX-314 Activates and Permeates Human TRPV1 and TRPA1 to Produce Inhibition of Sodium Channels and Cytotoxicity. Anesthesiology, 2016, 124(5): 1153-1165. 2. Binshtok AM, Bean BP, Woolf CJ. Inhibition of nociceptors by TRPV1-mediated entry of impermeant sodium channel blockers. Nature, 2007, 449(7162): 607-610.