Risperidone mesylate

本产品仅供科学实验研究使用! 不能用于临床或动物诊断！

产品名称	Risperidone mesylate	产品货号	CS-01Y77098
规格	10mg 50mg 100mg	CAS号	666179-96-0
含量	>98.00%	分子式	C24H31FN4O5S
分子量	506.59	用途	仅供科研研究使用

化学性质:       

   
Risperidone mesylate规格：10mg 50mg 100mg
CAS：666179-96-0
别名：N/A
化学名：N/A
分子式：C24H31FN4O5S

分子量：506.59
溶解度：Soluble in DMSO
储存条件：Store at -20°C
General tips：For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the   ultrasonic bath for a while.
Shipping Condition: Evaluation sample solution : ship with blue ice All other available size: ship with RT , or   blue ice upon request
产品描述: 

 
Risperidone mesylate(R 64 766 mesylate) is a serotonin 5-HT2 receptor blocker(Ki= 0.16 nM) and a potent dopamine D2 receptor antagonist(Ki= 1.4 nM). IC50 Value: 0.16 nM (Ki for 5-HT2 receptor); 1.4 nM (Ki for dopamine D2 receptor ) [1]Target: 5-HT2 receptor; D2 receptorRisperidone is an atypical antipsychotic drug which is mainly used to treat schizophrenia (including adolescent schizophrenia) and schizoaffective disorder. Risperidone has excellent oral activity, a rapid onset, and a 24-h duration of action.in vitro: Risperidone is serotonin 5-HT2 receptor blockade as shown by displacement of radioligand binding (Ki: 0.16 nM), activity on isolated tissues (EC50: 0.5 nM). Risperidone is also a potent dopamine D2 receptor antagonist as indicated by displacement of radioligand binding (Ki: 1.4 nM), activity in isolated striatal slices (IC50: 0.89 nM) [1]. Risperidone increased the production of IL-10 and MDC as well as the proinflammatory cytokines, such as IL-6, IL-8, and TNF-α, but decreased the production of IP-10 and IL-12. Furthermore, the exposure of DCs to risperidone led to lower IFN-γ production by T-cells [2].in vivo: Risperidone has the antagonism of peripherally (ED50: 0.0011 mg/kg) and centrally (ED50: 0.014 mg/kg) acting 5-HT2 receptor agonists in rats and antagonism of peripherally (ED50: 0.0057 mg/kg in dogs) and centrally acting D2 receptor agonists (ED50: 0.056-0.15 mg/kg in rats) [1]. Long-Evans rats received daily subcutaneous injections of vehicle or 1 of 2 doses of risperidone (1.0 and 3.0 mg/kg per day) from postnatal Days 14 to 42. Weight gain during development was slightly yet significantly reduced in risperidone-treatedrats. In the first 2 experiments, early-life risperidone administration was associated with increased locomotor activity at 1 week postadministration through approximately 9 months of age, independent of changes in weight gain [3].Toxicity: The changes in the reproductive system (uterus, ovary, vagina, cervix, and mammary gland) were considered secondary to the prolactin elevation, and the congestion of spleen was related to risperidone [4].[1]. Zhu HJ, et al. Risperidone and paliperidone inhibit p-glycoprotein activity in vitro. Neuropsychopharmacology. 2007 Apr;32(4):757-64. [2]. Chen ML, et al. Risperidone modulates the cytokine and chemokine release of dendritic cells and induces TNF-α-directed cellapoptosis in neutrophils. Int Immunopharmacol. 2012 Jan;12(1):197-204. [3]. Bardgett ME, et al. Adult rats treated with risperidone during development are hyperactive. Exp Clin Psychopharmacol. 2013 Jun;21(3):259-67. [4]. Tian J, et al. A 12-week intramuscular toxicity study of risperidone-loaded microspheres in Beagle dogs. Hum Exp Toxicol. 2013 Aug 7
使用方法: 

 
1. 常用筛选浓度
　　注意：用来筛选稳转株的工作浓度需要根据细胞类型，培养基，生长条件和细胞代谢率而变化，推荐使用浓度为50-1000μg/mL。对于第一次使用的实验体系建议通过建立杀灭曲线(kill curve)，即剂量反应性曲线，来确定最佳筛选浓度。
　　一般而言，哺乳动物细胞50-500μg/mL;细菌/植物细胞20-200μg/mL;真菌300-1000μg/mL。
2. 杀灭曲线的建立
　　注意：为了筛选得到稳定表达目的蛋白的细胞株，需要确定能够杀死未转染宿主细胞的抗生素浓度，可通过建立杀灭曲线(剂量反应曲线)来实现，至少选择5个浓度。
1) 第一天：未转化的细胞按照20-25%的细胞密度铺在合适的培养板上，37℃，CO2培养过夜;注：对于需要更高密度来检测活力的细胞，可增加接种量。
2) 根据细胞类型，设定合适范围内的浓度梯度。以哺乳动物细胞为例，可设定50，100，250，500，750，1000μg/mL。先用去离子水或者PBS buffer按照1:10的比例将母液稀释到5 mg/ml，然后按照下表稀释到相应浓度的工作液。
3) 第二天：替换旧的培养基，换用新鲜配制的含有相应浓度药物的培养基。每个浓度做三个平行孔。
4) 接下来每3-4天更换新的含药物培养基。
5) 按照固定的周期(如每2天)进行活细胞计数来确定阻止未转染细胞生长的恰当浓度。选择在理想的天数(通常是7-10天)内能够杀死绝大多数细胞的浓度为稳定转染细胞筛选用的工作浓度。
3. 稳定转染细胞的筛选
1) 转染48h后，用含有适当浓度的潮霉素B筛选培养基来传代细胞(直接传代或者稀释后传代)。
　　注意：细胞处于活跃分裂状态时抗生素的杀伤。则当细胞过于稠密，其效率会降低。为了得到较好的筛选效果，最好将细胞稀释至丰度不超过25%
2) 每隔3-4天更换含有药物的筛选培养液。
3) 筛选7天后观察并评估细胞克隆(集落)的形成情况。集落的形成可能还需要一周或者更多的时间，这取决于宿主细胞类型，转染，以及筛选效果。
4) 挑取并转移5-10个抗性克隆于35mm细胞培养板，继续用含药物的筛选培养液维持培养7天。
5) 之后更换正常培养基培养即可。
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蛋白酶抑制剂混合物实验步骤: 

 
(1)实验开始前将RNA提取液于65℃水浴锅中预热,离心管中加入ME(巯基乙醇),(10mL加80ul,50mL中加入300ul)
(2)取约0.8g菌丝体(液体培养获得的菌丝用真空抽滤即可！固体培养就更好说了),在液氮中迅速磨成精细粉末,装入50mL离心管,按1g材料8mL的量加入预热的RNA提取液,颠倒混匀
(3)65℃水浴3-10 min,期间混匀2-3次
(4)加入等体积的酚(注意是酸酚pH4.5)::yi戊醇(25:24:1)抽提(10,000rpm,4℃,5 min)
(5)取上清,等体积的yi戊醇(24:1)抽提(10,000rpm,4℃,5 min)
(6)加入1/4V体积10M LiCl溶液,4℃放置6h以上(或过夜)
(7)10,000rpm,4℃离心20min
(8)弃上清,用500ul SSTE溶解沉淀
(9)酚::yi戊醇(25:24:1)抽提两次,:yi戊醇(24:1)抽提1次(10,000rpm,4℃,5min)
(10)加2V体积的无水乙醇,在-70℃冰箱沉淀30min以上
(11)12,000rpm,4℃离心20 min
(12)弃上清.沉淀用70%酒精漂洗一次,干燥
(13)加200ul的DEPC处理水溶解
(14)用非变性琼脂糖凝胶电泳和紫外分光光度计扫描检测RNA的质量(在抽提过程中,若蛋白质含量或其它的杂质还较多,可以增加抽提次数)