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Pirenzepine

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货号 T61228Cas号 28797-61-7

Pirenzepine (LS 519 free base) is a selective antagonist of the M1 muscarinic acetylcholine receptor (mAChR). It effectively inhibits gastric acid secretion and reduces muscle spasm, making it a valuable compound for investigating peptic ulcers. Additionally, Pirenzepine exhibits anti-proliferative activity against cancer cells [1] [2].

Pirenzepine
其他形式的 “Pirenzepine”:

Pirenzepine

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Rating icon 还可以
货号 T61228Cas号 28797-61-7

Pirenzepine (LS 519 free base) is a selective antagonist of the M1 muscarinic acetylcholine receptor (mAChR). It effectively inhibits gastric acid secretion and reduces muscle spasm, making it a valuable compound for investigating peptic ulcers. Additionally, Pirenzepine exhibits anti-proliferative activity against cancer cells [1] [2].

规格价格库存数量
25 mg
¥ 10,600
5日内发货
50 mg
¥ 13,800
5日内发货
100 mg
¥ 17,500
5日内发货
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产品介绍


生物活性
产品描述
Pirenzepine (LS 519 free base) is a selective antagonist of the M1 muscarinic acetylcholine receptor (mAChR). It effectively inhibits gastric acid secretion and reduces muscle spasm, making it a valuable compound for investigating peptic ulcers. Additionally, Pirenzepine exhibits anti-proliferative activity against cancer cells [1] [2].
体外活性

Pirenzepine (100-140 μg/mL; 24 h) inhibits PC-3 cell proliferation activity [2]. Pirenzepine (110 μg/mL; 24 h) inhibits prostate and lung cancer cell migration [2]. Pirenzepine (100-130 μg/mL; 0-24 h) inhibits the expression of GLI1 in PC-3 cells [2]. Cell Proliferation Assay [2] Cell Line: PC-3 cells Concentration: 100-140 μg/mL Incubation Time: 24 hours Result: Inhibited PC-3 cell proliferation in a concentration-dependent manner. Cell Migration Assay [2] Cell Line: PC-3 and A549 cells Concentration: 110 μg/mL Incubation Time: 24 hours Result: Inhibited the migration of PC-3 and A549 cell lines (P=0.014). Western Blot Analysis [2] Cell Line: PC-3 cells Concentration: 110 μg/mL Incubation Time: 0-24 hours Result: Inhibited the expression of GLI1 and PTCH1. RT-PCR [2] Cell Line: PC-3 cell Concentration: 100-130 μg/mL Incubation Time: 24 hours Result: Suppressed GLI1 mRNA expression in PC-3 cells. Increased PTCH1 mRNA level but not reach statistical significance. Showed no SHH mRNA expression level change.

体内活性

Pirenzepine (intraperitoneal injection; 0.3 mg/kg; once) treatment shows beneficial effects in lipopolysaccharide-induced septic shock [3]. Animal Model: Male C57BL/6 mice with experimental endotoxemia [3] Dosage: 0.3 mg/kg Administration: Intraperitoneal injection; 0.3 mg/kg; once Result: Improved survival rate of LPS-induced septic shock. Relieved LPS-induced pulmonary and hepatic injury. Reduced the expression of SOCS3 at mRNA level.

化学信息
分子量351.4
分子式C19H21N5O2
CAS No.28797-61-7
SmilesC(CN1CCN(C)CC1)(=O)N2C=3C(NC(=O)C=4C2=CC=CC4)=CC=CN3
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

计算器

  • 摩尔浓度 计算器
  • 稀释 计算器
  • 配液 计算器
  • 分子量 计算器

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法:
比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL, 一共给药动物10只,您使用的配方为 10% DMSO + 40% PEG300 + 5% Tween 80 + 45% Saline / PBS / ddH2O, 那么您的工作液浓度为2 mg/mL
母液配置方法:2 mg 药物溶于 100 μL DMSO ( 母液浓度为 20 mg/mL ), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:100 μL DMSO 母液, 添加 400 μL PEG300 混匀澄清, 再加 50 μL Tween 80, 混匀澄清, 再加 450 μL Saline / PBS / ddH2O 混匀澄清
以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。
方案所需的各类助溶剂如: DMSOPEG300PEG400Tween 80SBE-β-CD玉米油等, 均可在TargetMol网站点击购买。
1 请输入动物实验的基本信息
mg/kg
g
μL
2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

剂量转换

对于不同动物的给药剂量换算,您也可以参考 更多

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