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利血平盐酸盐  ≥98%

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包装规格：100mg in glass bottle
溶解性：溶于DMSO（≥100mg/ml)
产品描述：基本信息 产品编号： R10377 产品名称： Reserpine hydrochloride CAS: 16994-56-2   储存条件 粉末 -20℃ 四年 分子式： C33H41ClN2O9 溶于液体 -80℃(密封储存) 6个月 分子量： 645.14 -20℃(密封储存) 1个月 化学名：  methyl (1R,15S,17R,18R,19S,20S)-6,18-dimethoxy-17-(3,4,5-trimethoxybenzoyl)oxy-1,3,11,12,14,15,16,17,18,19,20,21-dodecahydroyohimban-19-carboxylate;hydrochloride Solubility (25°C)：   体外:   DMSO   Ethanol   Water   体内(现配现用):   ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 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。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 1.5501mL 7.7503mL 15.5005mL 5mM 0.3100mL 1.5501mL 3.1001mL 10mM 0.1550mL 0.7750mL 1.5501mL   生物活性 产品描述 一种囊泡单胺转运蛋白2(VMAT2)的抑制剂。 靶点 VMAT2   体外研究 Reserpine hydrochloride is an inhibitor of the vesicular monoamine transporter 2 (VMAT2).Reserpine hydrochloride displays a significant on the density of dopamine D1 receptors (F2,12=8.81,p<0.01) in the rat striatum.The affinity (Kd) for the dopamine D1 and D2 receptors during withdrawal from acute and chronic administration of reserpine is not change.IC50 values of 43.9 and 54.9μM are obtained after 1 day of treatment with Reserpine hydrochloride in JB6 P+ and HepG2-C8 cells,respectively.Reserpine hydrochloride induces luciferase activity in a dose-dependent manner at concentrations ranging from 5 to 50μM,and no significant induction is observed at concentrations lower than 5μM.Results demonstrate that Reserpine hydrochloride (2.5 to 10μM) also increases the protein expression of Nrf2,HO-1,and NQO1.Reserpine hydrochloride at concentrations of 2.5 to 10μM decreases the mRNA expression of DNMT1,DNMT3a,and DNMT3b in a concentration-dependent manner in JB6 P+ cells after 7 days of treatment.Reserpine hydrochloride at 10μM generates a significant difference for DNMT3a expression (p<0.05). 体内研究 Withdrawal (48h) from chronic (14-day) but not acute Reserpine hydrochloride administration in a dose of 0.2mg/kg i.p.produces a significant reduction of the immobility time (F2,18=3.68,p<0.05),but increases the climbing time (F2,18=4.48,p<0.02),and does not change the swimming time (F2,18=1.78;NS) in the forced swim test (FST) in rats.Reserpine hydrochloride at a dose of 5mg/kg body weight produces significant increase in the urinary excretion profile of vanillylmandelic acid (VMA) compare to control animals.The amount of 5-hydroxyindoleacetic acid (5-HIAA) excreted in animals treated with Reserpine is found to be more than in the control.Dose dependent hypotension is observed with Reserpine hydrochloride.Reserpine hydrochloride at doses of 0.5,1,5,10 and 15μg/kg produce significant (p<0.01) reduction in blood pressure compare to control.   推荐实验方法(仅供参考) 激酶实验： After incubation for 24h,JB6 P+ cells (1×105 cells/10-cm dish) are treated with various concentrations of Reserpine hydrochloride.Whole cell lysates are prepared from the treated cells using radioimmunoprecipitation assay buffer supplemented with a protease inhibitor cocktail,and a BCA kit is used to determine protein concentrations.   细胞实验:   JB6 P+ cells are seeded in 96-well plates containing Minimum essential media (MEM) at a density of 1×104 cells/mL (100μL/well) for 1,3,and 5 days,and HepG2-C8 cells are seeded in plates containing DMEM.After incubation for 24h,the cells are treated with either DMSO or various concentrations of Reserpine hydrochloride.For JB6 P+ cells,the medium is changed every 2 days for the 3-day and 5-day treatments.Cell viability is assessed using a MTS assay kit according to the manufacturer’s instructions.The absorbance of the formazan product is read at 490nm,and the cell viability is calculated and compared with the DMSO control group.   动物实验:   Albino rats of either sex weighing between 100 to 150g are used in the study.They are acclimatized to the laboratory conditions for at least 10 days prior to the experiment and are provided with standard diet and water ad libitum with 12h light and dark cycle.Animals are divided into different groups of six each and are housed individually in metabolic cages.Group 1:Control animals treated with DMSO intraperitoneally at a dose of 0.1mL/100g body weight.Group 2:Animals administered intraperitoneally with Reserpine hydrochloride at a dose of 5mg/kg body weight.The 24h urine samples from the point of drug administration are collected for each animal.
保存条件：-20℃

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