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Rapacuronium bromide  ≥98%

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包装规格：1mg 5mg 10mg 25mg 50mg 100mg in glass bottle
溶解性：溶于DMSO(≥125mg/mL）
产品描述：基本信息 产品编号： R60006 产品名称： Rapacuronium bromide CAS: 156137-99-4   储存条件 粉末 -20℃ 四年   分子式： C37H61BrN2O4 溶于液体 -80℃ 6个月 分子量： 677.80 -20℃ 1个月 化学名：  1-((2S,3S,5S,8R,9S,10S,13S,14S,16S,17R)-3-acetoxy-10,13-dimethyl-2-(piperidin-1-yl)-17-(propionyloxy)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl)-1-allylpiperidin-1-ium bromide 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 1.4754mL 7.3768mL 14.7536mL 5mM 0.2951mL 1.4754mL 2.9507mL 10mM 0.1475mL 0.7377mL 1.4754mL   生物活性 产品描述 一种毒蕈碱性乙酰胆碱受体 (mAChR) 的变构调节剂。1-((2S,3S,5S,8R,9S,10S,13S,14S,16S,17R)-3-acetoxy-10,13-dimethyl-2-(piperidin-1-yl)-17-(propionyloxy)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl)-1-allylpiperidin-1-ium bromide 靶点 Muscarinic receptor   体外研究 Rapacuronium binds to all muscarinic receptor subtypes at physiologically relevant concentrations and displays micromolar affinity and slight selectivity towards M2 receptor.Rapacuronium exhibits complex effects on the kinetics of ACh binding and subsequent receptor activation estimated from stimulation of [35S]GTPγS binding.Rapacuronium alone concentration dependently lowers [35S]GTPγS binding to membranes with a maximal effect of approximately 25% at odd-numbered subtypes and 15% at even-numbered subtypes, with EC50 ranging from 28μM at M2 receptors to 76μM at M3 receptors.While the EC50 values of Rapacuronium in inhibiting [35S]GTPγS binding at individual subtypes correlated with affinities measured in binding experiments with [3H]ACh (R2=0.76) they are lower (4- to 12-fold) at all subtypes.Measurements of ACh-stimulated [35S]GTPγS binding in the presence of 0.1, 1 and 10μM Rapacuronium shows differential effects of Rapacuronium on receptor activation by an orthosteric agonist at individual receptor subtypes.At even-numbered subtypes 1μM and 10μM Rapacuronium significantly increases ACh EC50,with lowering of EMAX at 10μM Rapacuronium. At this subtype 0.1 and 1μM Rapacuronium causes a significant 2-fold decrease in ACh EC50 and approximately 60% and 35% increase in EMAX,respectively. Rapacuronium at 10μM increases ACh EC50 by about 3-fold without a significant change in EMAX.Rapacuronium (0.1-10μM) has no effect on ACh efficacy at the M1 and M5 subtypes but decreases the EC50 of ACh in stimulating [35S]GTPγS binding by 1.5- and 4-fold, respectively, at concentrations of 0.1 and 1μM.However,this effect is not evident at 10μM Rapacuronium. 体内研究 Time course of the neuromuscular effects of Rapacuronium following the administration of the 2×ED90 doses to rats and guinea-pigs with ED90 of 5953±199 and 187±16 µg/kg in rat and guinea pig, respectively.   推荐实验方法(仅供参考) 激酶实验： For determination of [35S]GTPγS binding to G-proteins in membranes a final concentration of 200pM (M1,M3 and M5 receptors) or 500pM (M2 and M4 receptors) of [35S]GTPγS is used.Incubation medium is supplemented with 5μM (M1,M3 and M5 receptors) or 50μM (M2 and M4 receptors) GDP.Nonspecific binding is determined in the presence of 1μM unlabeled GTPγS.When effects of Rapacuronium on ACh-stimulated [35S]GTPγS binding is measured Rapacuronium is added to membranes 60 min prior to ACh and [35S]GTPγS.Incubation with [35S]GTPγS is carried out for 20 min and free ligand is removed by filtration as described above.Filtration and washing with ice-cold water lasted for 9s (wash-aspirate button time).After filtration filters are dried in vacuum for 1 h while heated at 80℃ and then solid scintillator Meltilex A is melted on filters (105℃,90s) using a hot plate. After cooling the filters are counted using a Wallac Microbeta scintillation counter.
保存条件：-20℃

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