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Quinidine hydrochloride monohydrate Sale

(Synonyms: 奎尼丁盐酸盐一水合物) 目录号 : GC37062

An antiarrhythmic agent

Quinidine hydrochloride monohydrate Chemical Structure

Cas No.:6151-40-2

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥495.00
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100mg
¥450.00
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Sample solution is provided at 25 µL, 10mM.

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实验参考方法

Cell experiment:

Mouse (m) Slo3 (KCa5.1) channels or mutant forms are expressed in Xenopus oocytes and currents recorded with 2-electrode voltage-clamp. Gain-of-function mSlo3 mutations are used to explore the state-dependence of the inhibition. The interaction between Quinidine hydrochloride monohydrate and mSlo3 channels is modelled by in silico docking[1].

Animal experiment:

24 rats are randomly divided into three groups with eight rats in each group. Groups Q1, Q3, and Q5 receive Quinidine hydrochloride monohydrate 1, 3, and 5 μmol, respectively, in 5 % glucose 0.1 mL. The sciatic nerve is exposed by making an incision from the left sciatic notch to the distal thigh. The subcutaneous tissue is bluntly dissected to expose the biceps femoris. The sciatic nerve is freed from its investing fascia. The procedure is then repeated on the right side. The somato-sensory evoked potential (SSEP) and compound muscle action potentials (CMAP) are recorded at baseline, immediately after Quinidine hydrochloride monohydrate treatment, then every 15 min thereafter for 1 h, then every 30 min thereafter for 3 h. The animals are allowed to recover and then kept separately for 2 weeks. After performing behavioral examinations, electrophysiological examinations are performed with the animals under intra-peritoneal anesthesia[2].

References:

[1]. Wrighton DC, et al. Mechanism of inhibition of mouse Slo3 (KCa 5.1) potassium channels by quinine, quinidine and barium. Br J Pharmacol. 2015 Sep;172(17):4355-63.
[2]. Cheng KI, et al. Application of quinidine on rat sciatic nerve decreases the amplitude and increases the latency of evoked responses. J Anesth. 2014 Aug;28(4):559-68.

产品描述

Quinidine is a stereoisomer of the antimalarial agent quinine and a class Ia antiarrhythmic agent.1,2 Quinidine blocks the voltage-gated sodium (Nav) channel Nav1.5 in a use-dependent manner.1 It decreases the amplitude and duration of action potentials in isolated canine ventricular myocytes.3 It inhibits KKr, peak INa, and late INa (IC50s = 4.5, 11, and 12 ?M, respectively) and can induce torsade de pointes in isolated rabbit hearts when used at a concentration of 1 ?M.2 Quinidine induces QT prolongation in dogs.4 It also binds to M2 muscarinic acetylcholine receptors (Ki = 7.5 ?M for human recombinant receptors expressed in HM2-B10 cells).5 Formulations containing quinidine have been used in the treatment of atrial fibrillation and ventricular arrhythmias.

1.Roden, D.M.Pharmacology and toxicology of Nav1.5-class 1 anti-arrhythmic drugsCard. Electrophysiol. Clin.6(4)695-704(2014) 2.Wu, L., Guo, D., Li, H., et al.Role of late sodium current in modulating the proarrhythmic and antiarrhythmic effects of quinidineHeart Rhythm5(12)1726-1734(2008) 3.Salata, J.J., and Wasserstrom, J.A.Effects of quinidine on action potentials and ionic currents in isolated canine ventricular myocytesCirc. Res.62(2)324-337(1988) 4.Rakhit, A., Guentert, T.W., Holford, N.H.G., et al.Pharmacokinetics and pharmacodynamics of quinidine and its metabolite, quinidine-N-oxide, in beagle dogsEur. J. Drug Metab. Pharmacokinet.9(4)315-324(1984) 5.Kovacs, I., Yamamura, H.I., Waite, S.L., et al.Pharmacological comparison of the cloned human and rat M2 muscarinic receptor genes expressed in the murine fibroblast (B82) cell lineJ. Pharmacol. Exp. Ther.284(2)500-507(1998)

Chemical Properties

Cas No. 6151-40-2 SDF
别名 奎尼丁盐酸盐一水合物
Canonical SMILES C=C[C@H]1C[N@](CC[C@H]1C2)[C@@]2([H])[C@@H](O)C3=CC=NC4=CC=C(OC)C=C34.[H]Cl.[H]O[H]
分子式 C20H27ClN2O3 分子量 378.89
溶解度 DMSO: 100 mg/mL (263.93 mM); Water: 2.5 mg/mL (6.60 mM) 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.6393 mL 13.1964 mL 26.3929 mL
5 mM 0.5279 mL 2.6393 mL 5.2786 mL
10 mM 0.2639 mL 1.3196 mL 2.6393 mL
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