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 普卡必利Prucalopride
分子式：C18H26ClN3O3   分子量：367.87
 质量标准：>98%，5-HT 受体激动剂
产品描述
Prucalopride 是选择性，高亲和力5-HT 受体激动剂，作用于5-HT4A和5-HT4B受体，Ki分别为2.5 nM 和 8 nM, 比作用于5-HT受体亚型选择性高290倍以上。
靶点
5-HT4a
5-HT4b
      
IC50
2.5 nM (Ki)
8 nM (Ki)
      
体外研究
Prucalopride induces contractions in a concentration-dependent manner with pEC50 of 7.5. Prucalopride (1 mM) significantly amplifies the rebound contraction of the guinea-pig proximal colon after electrical field stimulation. Prucalopride induces relaxation of the rat oesophagus preparation of rat oesophagus tunica muscularis mucosae with pEC50 of 7.8, yielding a monophasic concentration–response curve.
体内研究
Complete bowel movements per week is 30.9% of those receiving 2 mg of Prucalopride ａnd 28.4% of those receiving 4 mg of Prucalopride, as compared with 12.0% in the placebo group. 47.3% of patients receiving 2 mg of Prucalopride ａnd 46.6% of those receiving 4 mg of Prucalopride has an increase in the number of spontaneous, complete bowel movements of one or more per week, on average, as compared with 25.8% in the placebo group. Prucalopride (2 mg or 4 mg) significantly improves all other secondary efficacy end points, including patients＇ satisfaction with their bowel function ａnd treatment ａnd their perception of the severity of their constipation symptoms.Prucalopride (4 mg daily) accelerates overall gastric emptying ａnd small bowel transit in patients with constipation without a rectal evacuation disorder. Prucalopride (4 mg daily) tends to accelerate overall colonic transit with significantly faster overall colonic transit ａnd ascending colon emptying.Higher proportions of patients on prucalopride 2 mg (19.5%), 4 mg (23.6%) has three or more spontaneous complete bowel movements(SCBM)/week compared with placebo (9.6%). Prucalopride also significantly improves secondary efficacy ａnd quality of life endpoints, including the proportion of patients with an increase of one or more SCBM/week, evacuation completeness, perceived disease severity ａnd treatment effectiveness ａnd quality of life.Prucalopride alters colonic contractile motility patterns in a dose-dependent fashion by stimulating high-amplitude clustered contractions in the proximal colon ａnd by inhibiting contractile activity in the distal colon of fasted dogs. Prucalopride also causes a dose-dependent decrease in the time to the first giant migrating contraction (GMC); at higher doses of prucalopride, the first GMC generally occurres within the first half-hour after treatment.
溶解性
DMSO 60 mg/mL，水 <1 mg/mL，乙醇 38 mg/mL
稳定性
2年 -20°C粉状，6月-80°C溶于DMSO
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任何试剂严禁用手直接触摸及用嘴尝，酸性或碱性液体溅至皮肤不得用中和剂处理，防止放热烧伤。
上海普卡必利179474-81-8价格供应常见问题
1，取用药品时要做到三不原则：不能用手接触药品。不要把鼻孔凑到容器口直接去闻药品的气味，应用手在瓶口轻轻煽动，仅使少量气味进入鼻孔。不得品尝药品。
　　2，注意节约药品。如果没有说明用量，一般取少量。液体取用1-2ml，固体只需盖满试管底部。
　　3，实验完毕后，剩余药品要做到三不一要，即不放回原瓶，不随意丢弃，不拿出实验室。一要，要放入指定容器内。
　　4，固体药品的取用。块状用镊子，粉末用药匙（或纸槽）。取固体应做到“一横二送三慢竖”以免打破试管底。用粉末时应做到“一斜二送三直立”
　　5，液体药品的取用。1，应把瓶塞拿下，倒放在实验台上防止污染溶液。2，倾倒时标签应向着手心，以免腐蚀标签。3，瓶口紧挨试管口。取少量时，应用胶头滴管滴加，滴加时要保持垂直悬空滴加，不能伸入瓶内或试管内，防止污染试剂。取一定量时，常用量筒量出体积，量筒必须放平，读数时，事先要与量筒内凹液面处保持水平。