Quinidine hydrochloride monohydrate
(Synonyms: 奎尼丁盐酸盐一水合物) 目录号 : GC37062
An antiarrhythmic agent
Cas No.:6151-40-2
Sample solution is provided at 25 µL, 10mM.
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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)
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. | |
| 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 |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 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。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet