盐酸尼卡地平作用机制 - Medchemexpress - MCE中国

1、Product Data SheetNicardipine hydrochlorideCat. No.: HY-12515ACAS No.: 54527-84-3分式: CHClNO分量: 515.99作靶点: Calcium Channel; Autophagy作通路: Membrane Transporter/Ion Channel; Neuronal Signaling; Autophagy储存式: 4C, protect from light* In solvent : -80C, 6 months; -20C, 1 month (protect from light)溶解性数据体外实

2、验 DMSO : 35 mg/mL (67.83 mM)* means soluble, but saturation unknown.SolventMass1 mg 5 mg 10 mgConcentration制备储备液1 mM 1.9380 mL 9.6901 mL 19.3802 mL5 mM 0.3876 mL 1.9380 mL 3.8760 mL10 mM 0.1938 mL 0.9690 mL 1.9380 mL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；旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存式和期限：-80C, 6 months; -20

3、C, 1 month (protect from light)。-80C 储存时，请在 6 个内使，-20C 储存时，请在 1 个内使。体内实验请根据您的实验动物和给药式选择适当的溶解案。以下溶解案都请先按照 In Vitro 式配制澄清的储备液，再依次添加助溶剂：为保证实验结果的可靠性，澄 的储备液可以根据储存条件，适当保存；体内实验的作液，建议您现现配，当天使； 以下溶剂前显的百分 指该溶剂在您配制终溶液中的体积占；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的式助溶1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

4、Solubility: 2.5 mg/mL (4.85 mM); Clear solution此案可获得 2.5 mg/mL (4.85 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 400 L PEG300 中，混合均匀；向上述体系中加50 L Tween-80，混合均匀；然后继续加 450 L 理盐定容 1 mL。2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (4.85 mM); Clear solution此案可获得

5、2.5 mg/mL (4.85 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 900 L 20% 的 SBE-CD 理盐溶液中，混合Page 1 of 2 www.MedChemE均匀。BIOLOGICAL ACTIVITY物活性 Nicardipine hydrochloride (YC-93)种钙通道 (calcium channel) 阻滞剂，可阻断脏钙通道，IC50 为 1 M。Nicardipine hydrochloride 可于治疗慢性绞痛以及控制压1。IC & Target IC50: 1 M (car

6、diac calcium channels)1体外研究 Nicardipine (0.1-10 M; 24-48 h) reduces viability and proliferation of vascular smooth muscle cells (VSMCs) andinhibits their ability to migrate2.Cell Viability Assay2Cell Line: VSMCs were isolated from New Zealand rabbit aortic preparationsConcentration: 0.1 M, 1 M, 3 M,

7、 10 MIncubation Time: 24-48 hoursResult: Treatment reduced significantly cell viability and inhibited VSMCs proliferation in thepresence of 10% FBS in a dose-dependent way, from 205.417.5% to 176.617%,160.65.7%, 150.411.2%, 61.227.83% after 0.1 M, 1 M, 3 M, 10 M treatment,respectively.Western Blot A

8、nalysis1Cell Line: BV-2 microglial cellsConcentration: 1, 3, 5, 10 MIncubation Time: 1 hoursResult: Reduced LPS/IFN- and peptidoglycan-induced iNOS expression and COX-2expression in a concentration-dependent manners.体内研究Nicardipine (0.3-10 mg/kg; p.o.) shows antihypertensive properties3.LD50s of Nic

9、ardipine are 643 mg/kg (oral) and 557 mg/kg (oral); 18.1 mg/kg (intravenous) 25.0 mg/kg (intravenous);735 mg/kg (subcutaneous) and 683 mg/kg (subcutaneous); 171 mg/kg (intraperitoneally) and 155 mg/kg(intraperitoneally) for male and female Sprague-Dawley rats, respectively3.LD50s of Nicardipine are

10、187 mg/kg (oral) and 15.5 mg/kg (intravenous) for male Wistar rats, respectively3.LD50s of Nicardipine are 634 mg/kg (oral) and 650 mg/kg (oral); 20.7 mg/kg (intravenous) 19.9 mg/kg (intravenous);540 mg/kg (subcutaneous) and 710 mg/kg (subcutaneous); 144 mg/kg (intraperitoneally) and 161 mg/kg(intra

11、peritoneally) for male and female mice, respectively3.Animal Model: In conscious normotensive rats (NR)3Dosage: 0.3-10 mg/kgAdministration: P.o.Result: Induced a dose-dependent hypotensive response (maximal decrease in mean bloodPage 2 of 3 www.MedChemEpressure, supine position) without any postural

12、 hypotensive response.户使本产品发表的科研献 Biosci Rep. 2019 Jun 20. Int J Clin Exp Med. 2019;12(5):5184-5190.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Charnet P, et al. Electrophysiological analysis of the action of nifedipine and nicardipine on myocardial fibers. Funda

13、m Clin Pharmacol. 1987;1(6):413-31.2. R Stamatiou, et al. The dihydropyridine calcium antagonist nicardipine reduces aortic smooth muscle cell viability, proliferation and migration.Cardiovascular Research, 2018 Apr,114(1):S43.3. Sherrin H. Baky. Nic ardipine Hydrochloride.McePdfHeightCaution: Product