Quinidine-hydrochloride-monohydrate _Potassium Channel 抑制劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEQuinidine hydrochloride monohydrateCat. No.: HY-B1302CAS No.: 6151-40-2分式: CHClNO分量: 378.89作靶點(diǎn): Potassium Channel作通路: Membrane Transporter/Ion Channel儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)

2、驗(yàn) DMSO : 106.7 mg/mL (281.61 mM; Need ultrasonic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.6393 mL 13.1964 mL 26.3929 mL5 mM 0.5279 mL 2.6393 mL 5.2786 mL10 mM 0.2639 mL 1.3196 mL 2.6393 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Quinidine hydrochlori

3、de monohydrate臨床抗律失常藥物，也是K+ 通道 (K+ channel) 的有效阻斷劑，其 IC50 值為 19.9 M。IC50 & Target IC50: 19.9 M (K+ channel) 1體外研究Quinidine hydrochloride monohydrate blocks WT mSlo3 (KCa5.1) channels with an IC50 of 19.91.41Mand Hill slope of 1.150.15 (n=7). Again, the potency of inhibition by Quinidine hydrochlorid

4、e monohydrate is1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEhigher for F304Y mSlo3 (IC50 of 2.420.60M, n=9, P50 of 38.46.77M, n=5, P 1.體內(nèi)研究 Direct application of Quinidine hydrochloride monohydrate on the sciatic nerve produces a dose-relateddecrease in amplitude at ascending somato-sensory evo

5、ked potential (SSEP) and descending compoundmuscle action potentials (CMAP) when comparing baseline with other time points, or when comparing theexperimental left limb to the right contra-lateral glucose-treated limb. The latencies of SSEPs and CMAPpotentials after Quinidine hydrochloride monohydrat

6、e applications are increased compare to baseline and thecontralateral side 2.PROTOCOLCell Assay 1 Mouse (m) Slo3 (KCa5.1) channels or mutant forms are expressed in Xenopus oocytes and currentsrecorded with 2-electrode voltage-clamp. Gain-of-function mSlo3 mutations are used to explore the state-depe

7、ndence of the inhibition. The interaction between Quinidine hydrochloride monohydrate and mSlo3channels is modelled by in silico docking 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal 24 rats are randomly divided into three groups with eight r

8、ats in each group. Groups Q1, Q3, and Q5 receiveAdministration 2 Quinidine hydrochloride monohydrate 1, 3, and 5 mol, respectively, in 5 % glucose 0.1 mL. The sciaticnerve is exposed by making an incision from the left sciatic notch to the distal thigh. The subcutaneous tissueis bluntly dissected to

9、 expose the biceps femoris. The sciatic nerve is freed from its investing fascia. Theprocedure is then repeated on the right side. The somato-sensory evoked potential (SSEP) and compoundmuscle action potentials (CMAP) are recorded at baseline, immediately after Quinidine hydrochloridemonohydrate tre

10、atment, then every 15 min thereafter for 1 h, then every 30 min thereafter for 3 h. Theanimals are allowed to recover and then kept separately for 2 weeks. After performing behavioralexaminations, electrophysiological examinations are performed with the animals under intra-peritonealanesthesia 2.MCE

11、 has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Environ Int. 2019 Jun;127:694-703. RSC Adv. 2019 May.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Wrighton DC, et al. Mechanism of inhibition of mouse Slo3 (KCa 5.1) potas

12、sium channels by quinine, quinidine and barium. Br JPharmacol. 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. JAnesth. 2014 Aug;28(4):559-68.McePdfHeight2/2 Master of Small Molecules 您邊的抑制劑師www.MedChemECaution: P