Prucalopride 普芦卡必利,99.83%

产品编号:Bellancom-14151| CAS NO:179474-81-8| 分子式:C18H26ClN3O3| 分子量:367.87

Prucalopride (R093877)是高亲和性5-HT4受体激动剂,对5-HT4a/4b的pKi分别为8.6/8.1,比对其它受体的亲和性高150倍。

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用,

货号 包装 价格 库存与货期 购买量 操作
Bellancom-14151
600.00 杭州 北京(现货)
Bellancom-14151
960.00 杭州 北京(现货)
Bellancom-14151
1680.00 杭州 北京(现货)

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Prucalopride 普芦卡必利

产品介绍 Prucalopride 是一种口服有效的,具有选择性和特异性的 5-HT 4 受体激动剂,对人 5-HT4a/4b 受体具有高亲和力,其 pKi 值分别为 8.6 和 8.1。Prucalopride 通过促进大鼠肠道神经系统的再生来改善肠道运动能力。Prucalopride 还能通过阻断 PI3K/AKT/mTor 信号通路发挥抗癌活性。Prucalopride 可用于慢性便秘相关的运动障碍,假性肠梗阻以及癌症的研究。
生物活性

Prucalopride is an orally active, selective and specific 5-HT 4 receptor agonist (high affinity), with pKis of 8.6 and 8.1 for human 5-HT4a/4b receptors, respectively. Prucalopride improves intestinal motility by promoting regeneration of the intestinal nervous system in rats. Prucalopride also shows anticancer activity by blocking of the PI3K/AKT/mTor signaling pathway. Prucalopride can be used in studies of chronic constipation, pseudo-intestinal obstruction and cancer.

体外研究

Prucalopride (10 µM; 24, 48, 72 h) shows anti proliferative activity in A549 cells.
Prucalopride induces autophagy and apoptosis, decreases the expression of the phosphorylated protein kinase B (AKT) and mammalian target of rapamycin (mTor) in A549/A427 cells.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

Cell Line: A549 cells
Concentration: 10 µM
Incubation Time: 24, 48, 72 h
Result: Repressed lung cancer cells proliferation.
体内研究
(In Vivo)

Prucalopride (5, 10 µg/kg; p.o.; single daily for 2 weeks) shortens the colonic transit time in DM model, promotes the regeneration of colonic neural stem cells and neurons.
Prucalopride (5, 10 µg/kg; p.o.; single daily for 2 weeks) promotes the differentiation of colonic neural stem cells, activates the expression of glial proteins and promotes the recovery of neuronal injury to a certain extent.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Sprague dawley rats (diabetes mellitus (DM) model).
Dosage: 5 or 10 µg/kg
Administration: Oral gavage; single daily for 2 weeks.
Result: Accelerated colonic movement and shortened the colonic transit time, and markedly increased the expression levels of Ki67.
Increased expression of SOX10 in the columnar epithelial nuclei and enteraden (when at 5 µg/kg), and in the columnar epithelial cells, the nuclei of lamina propria cells and enteraden (when at 10 µg/kg).
Significantly increased Nestin expression, which concentrated in columnar epithelial cells and the mesenchyme. (Nestin:a marker of enteric neural stem cells in the ENS).
体内研究

Prucalopride (5, 10 µg/kg; p.o.; single daily for 2 weeks) shortens the colonic transit time in DM model, promotes the regeneration of colonic neural stem cells and neurons.
Prucalopride (5, 10 µg/kg; p.o.; single daily for 2 weeks) promotes the differentiation of colonic neural stem cells, activates the expression of glial proteins and promotes the recovery of neuronal injury to a certain extent.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Sprague dawley rats (diabetes mellitus (DM) model).
Dosage: 5 or 10 µg/kg
Administration: Oral gavage; single daily for 2 weeks.
Result: Accelerated colonic movement and shortened the colonic transit time, and markedly increased the expression levels of Ki67.
Increased expression of SOX10 in the columnar epithelial nuclei and enteraden (when at 5 µg/kg), and in the columnar epithelial cells, the nuclei of lamina propria cells and enteraden (when at 10 µg/kg).
Significantly increased Nestin expression, which concentrated in columnar epithelial cells and the mesenchyme. (Nestin:a marker of enteric neural stem cells in the ENS).
体内研究

Prucalopride (5, 10 µg/kg; p.o.; single daily for 2 weeks) shortens the colonic transit time in DM model, promotes the regeneration of colonic neural stem cells and neurons.
Prucalopride (5, 10 µg/kg; p.o.; single daily for 2 weeks) promotes the differentiation of colonic neural stem cells, activates the expression of glial proteins and promotes the recovery of neuronal injury to a certain extent.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Sprague dawley rats (diabetes mellitus (DM) model).
Dosage: 5 or 10 µg/kg
Administration: Oral gavage; single daily for 2 weeks.
Result: Accelerated colonic movement and shortened the colonic transit time, and markedly increased the expression levels of Ki67.
Increased expression of SOX10 in the columnar epithelial nuclei and enteraden (when at 5 µg/kg), and in the columnar epithelial cells, the nuclei of lamina propria cells and enteraden (when at 10 µg/kg).
Significantly increased Nestin expression, which concentrated in columnar epithelial cells and the mesenchyme. (Nestin:a marker of enteric neural stem cells in the ENS).
性状Solid
溶解性数据
In Vitro: 

H2O : 50 mg/mL (135.92 mM; Need ultrasonic)

DMSO : ≥ 31 mg/mL (84.27 mM)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7184 mL 13.5918 mL 27.1835 mL
5 mM 0.5437 mL 2.7184 mL 5.4367 mL
10 mM 0.2718 mL 1.3592 mL 2.7184 mL
*

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
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: PBS

    Solubility: 50 mg/mL (135.92 mM); Clear solution; Need ultrasonic

*以上所有助溶剂都可在 西域 网站选购。
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
参考文献

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符号 GHS07 GHS09
GHS07, GHS09
信号词 Warning
危害声明 H315-H319-H335-H400
警示性声明 P305 + P351 + P338
危险品运输编码 UN 3077 9 / PGIII
1. 物质的识别
产品名: Prucalopride
CAS号: 179474-81-8
制造商/供应商: 西域试剂
网站:www.hzbp.cn   邮件:13911702513@139.com
2. 合成/成分数据
产品名: Prucalopride
分子式: C18H26ClN3O3
分子量: 367.87
3. 急救措施
吸入后: 如果吸入,移至空气新鲜处,如果呼吸困难,给输氧,如呼吸停止,给予人工呼吸。
皮肤接触后: 用大量的水冲洗,移除污染的衣服和鞋子。
眼睛接触后: 检查并取下隐形眼镜,并用大量的水冲洗;呼叫医生。
吞食后: 如果吞食,用大量纯净水漱口;呼叫医生。
4. 消防措施
适当的灭火剂: 雾状水,二氧化碳,干粉或泡沫。
防护设备: 穿戴自给式呼吸器和防护服,以防止与皮肤和眼睛接触。
5. 泄漏应急处理
安全防范措施: 封锁泄漏区域;穿戴自给式呼吸器,防护服和厚橡胶手套。
清洁/收集措施: 使用液体粘合原料(硅藻土,通用粘合剂)吸取精细粉末;
使用酒精擦洗表面和设备除去污渍;
根据第11条处理被污染的材料。
6. 处理和储存
安全处理说明: 避免吸入和接触皮肤,眼睛及衣物;材料可能略微具有刺激性。
储存: 粉末型式       -20°C   3年;4°C   2年
溶于溶剂       -80°C   6个月;-20°C   1个月
7. 接触控制和个人防护
呼吸设备: NIOSH / MSHA认可的呼吸器。
双手保护: 耐化学腐蚀的橡胶手套。
眼睛防护: 化学安全护目镜。
8. 稳定性和反应活性
稳定性: 按照说明存储是稳定的;避免强氧化剂。
热分解/其他要避免的情况: 避免光和热。
9. 毒性资料
急性毒性: 无可用资料。
主要刺激性影响: 无可用资料。
在皮肤上: 无可用资料。
对眼睛: 无可用资料;可能具有刺激性。
10. 生态资料
一般注意事项: 无可用资料。
11. 废弃处置
按照所在国家,省份,县市和地方的法规处置。
12. 运输信息
正确的运输名称:
非危险品运输: 这种物质被视为非危险品运输。
13. 法规信息
尚未有针对此产品作出的化学安全性评估。
14. 其他信息
这种化学品仅供受过训练的,有经验的研究人员在穿戴适当装备和授权允许的情况下进行操作处理。以上信息基于我们目前的知识被认为是正确的,但只适用于作为有经验人员的指导。请咨询您自己的安全顾问,并遵守当地和国家的安全法规。在任何其他没有被警告的情况下,并不意味着绝对没有危险存在。西域生物技术不承担任何使用这种化学品所造成的损害和责任。2023 西域生物技术版权所有。





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