Quinidine - Parasite 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEQuinidineCat. No.: HY-B1751CAS No.: 56-54-2分式: CHNO分量: 324.42作靶点: Parasite作通路: Anti-infection储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 50 mg/mL (154.12 mM)H2O : 40% PEG300 5% Tween-80

2、 45% salineSolubility: 2.5 mg/mL (7.71 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (7.71 mM); Clear solution1/3 Master of Small Molecules 您边的抑制剂师www.MedChemE3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (7.71 mM); Clear solutionBIOLOGICAL ACTI

3、VITY物活性 Quinidine抗律失常药物，可治疗律失常，也可作疟疾的治疗。IC50 & Target Parasite 1体外研究 Quinidine is a clinical anti-arrythmic drug which affects ionic currents in heart muscle and which has alsobeen shown to be a potent blocker of several classes of K+ channel in a variety of cell types. Bath applicationof quinidine

4、causes a dose-dependent reduction of the peak amplitude of Ik. The Kd for blockade of Ik at 0mV is estimated to be 41 M. Quinidine elicits a dose-dependent increase of the rate of the decay of Ik andthis effect is enhanced by membrane depolarization. Quinidine also causes a 5 mV hyperpolarizing shif

5、t ofthe steady-state inactivation curve and increases the half-time for recovery from inactivation. Quinidine doesnot affect the onset of inactivation measured at -30 mV 1.体内研究 Quinidine sulfate is rapidly absorbed, with peak plasma concentrations 60-90 min after an oral dose. Othersalts (gluconate,

6、 polygalacturonate) are more slowly absorbed, with lower peak concentrations. Quinidine isapproximately 70-90 % bound to plasma proteins. It undergoes hepatic oxidative metabolism to form an N-oxide, a 3-hydroxy form, an O-demethyl form and 2-quinidinone. Over one-half of patients starting quinidine

7、stop within the first year of therapy because of side effects. These include, commonly, diarrhea, nausea, andvomiting which are not necessarily related to high plasma concentrations 2. Quinidine inhibits metabolism ofamphetamine in rats. Quinidine pretreatment results in a significant decrease in th

8、e excretion of p-hydroxyamphetamine at 24 and 48 h to 7.2 and 24.1% of the vehicle-control levels, respectively,accompanied by a significant increase in amphetamine excretion between 24 and 48 h to 542% of the control3.PROTOCOLAnimal Rats: Three rats are placed in individual metabolic cages with fre

9、e access to food and water. After 24 h, urineAdministration 3 is collected (0 h) and the rats receive the following treatment: (1) no treatment; (2) 80 mg quinidine/kg (po) at1.0 mL/kg, and (III) 50% ethanol (1.0 mL/kg). Two hours later, all three rats receive a single dose of 15 mgamphetamine/kg (p

10、o) at 1.0 mL/kg. Urine is then collected at 24 and 48 h after the administration ofquinidine. This procedure is repeated three times. After collection of urine, volume and pH are measured andthe urine is stored until analysis 3.MCE has not independently confirmed the accuracy of these methods. They

11、are for reference only.户使本产品发表的科研献 Environ Int. 2019 Jun;127:694-703. RSC Adv. 2019 May.2/3 Master of Small Molecules 您边的抑制剂师www.MedChemESee more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Kehl SJ, et al. Quinidine-induced inhibition of the fast transient outward K+ current in rat

12、melanotrophs. Br J Pharmacol. 1991Jul;103(3):1807-13.2. Roden DM, et al. Class I antiarrhythmic agents: quinidine, procainamide and N-acetylprocainamide, disopyramide.3. Moody DE, et al. Quinidine inhibits in vivo metabolism of amphetamine in rats: impact upon correlation between GC/MS andimmunoassay findings in rat urine. J Anal Toxicol. 1990 Sep-Oct;14(5):311-7.McePdfHeightCaution