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| 包装规格: | 5g in glass bottle |
| 溶解性: | 溶于DMSO(25mg/mL 超声) |
| 产品描述: | 基本信息 产品编号: U10085 产品名称: Urapidil CAS: 34661-75-1 储存条件 粉末 室温 四年 分子式: 34661-75-1 溶于液体 -80℃ 两年 分子量 387.48 -20℃ 1个月 化学名: 6-[[3-[4-(2-Methoxyphenyl)-1-piperazinyl]propyl]amino]-1,3-dimethyluracil Solubility (25°C): 体外: DMSO 77 mg/mL (198.71mM) Water Insoluble Ethanol ''77 mg/mL 体内(现配现用): 1.请依序添加每种溶剂:10% DMSO→40% PEG300→5% Tween-80→45% saline Solubility: ≥ 2.5 mg/mL (6.45mM); Clear solution 此方案可获得 ≥ 2.5 mg/mL (6.45mM,饱和度未知) 的澄清溶液。 以 1mL 工作液为例,取 100μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50μL Tween-80,混合均匀;然后继续加入 450μL生理盐水定容至 1mL。 2.请依序添加每种溶剂: 10% DMSO→90% (20% SBE-β-CD in saline) Solubility: ≥ 2.5 mg/mL (6.45mM); Clear solution 此方案可获得 ≥ 2.5 mg/mL (6.45mM,饱和度未知) 的澄清溶液。 以 1mL 工作液为例,取 100μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 3.请依序添加每种溶剂:10% DMSO→90% corn oil Solubility: ≥ 2.5 mg/mL (6.45mM); Clear solution 此方案可获得 ≥ 2.5 mg/mL (6.45mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1mL 工作液为例,取 100μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900μL玉米油中,混合均匀。 <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 2.5808mL 12.9039mL 25.8078mL 5mM 0.5162mL 2.5808mL 5.1616mL 10mM 0.2581mL 1.2904mL 2.5808mL 生物活性 产品描述 一种α1 肾上腺素受体的拮抗剂和 5-HT1A 受体的激动剂。 靶点 5-HT1A Receptor α1-adrenoreceptor 体外研究 Urapidil is an α1 adrenoreceptor antagonist and a 5-HT1A receptor agonist. Urapidil does not affect vascular tone at concentrations up to 10-5 M. Urapidil (10-5 M) markedly inhibits the alpha 1-adrenergic agonist (phenylephrine)-induced concentration-dependent contractions in aortic rings without endothelium and also to some extent in those with endothelium. Moreover, the inhibitory effect of Urapidil is more pronounced in rings without endothelium than in those with endothelium. Urapidil (10-5 M) affects neither the vascular tone nor the concentration-dependent contraction to serotonin 推荐实验方法(仅供参考) Cell Assay The rat aorta is placed in Krebs solution and stripped of connective tissue, then subsequently cut into rings (2 to 3 mm in length). As indicated, the endothelium is removed by rubbing the intimal surface of rings with a pair of forceps. The rings are suspended in organ baths containing oxygenated (95% O2 and 5% CO2) Krebs bicarbonate solution. Following equilibration for 90 min under a resting tension of 2 g, the rings are contracted with KCl (80mM) to assess their reactivity. After a 30-min washout period, the rings are contracted with the α1-adrenergic receptor agonist phenylephrine (10-6 M) to about 80% of the maximal contraction before addition of acetylcholine (10-6 M) to check for the presence of a functional endothelium. After a 30-min equilibration period, the rings with or without endothelium are exposed to Urapidil (10-5 M) for 25 min before inducing a concentration-contraction curve to phenylephrine |
| 保存条件: | 室温 |
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