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S84820

Pirenzepine dihydrochloride

源叶(MedMol) 99%
  • 英文名:
  • Pirenzepine dihydrochloride
  • 别名:
  • 盐酸哌仑西平;哌伦西平; 5,11-二氢-11-[(4-甲基-1-哌嗪基)乙酰]-6H-吡啶并[2,3-b][1,4]苯并二氮卓-6-酮二盐酸盐;;Pirenzepine hydrochloride; Pirenzepine dihydrochloride; Pirenzepine dihydrochloride monohydrate;
  • CAS号:
  • 29868-97-1
  • 分子式:
  • C19H21N5O2?2HCl
  • 分子量:
  • 424.32
  • MDL:
  • MFCD00055214
  • 核磁/质谱:
品牌货号产品规格价格(RMB) 库存(上海) 北京 武汉 南京 数量计量单位 加入购物车...
源叶(MedMol) S84820-25mg 99% ¥50.00元 3 - - - EA 加入购物车
源叶(MedMol) S84820-100mg 99% ¥120.00元 8 - - - EA 加入购物车
源叶(MedMol) S84820-500mg 99% ¥400.00元 6 - - - EA 加入购物车
源叶(MedMol) S84820-1g 99% ¥700.00元 5 - - - EA 加入购物车
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  • 产品描述: Pirenzepine (LS 519) dihydrochloride is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist. Pirenzepine dihydrochloride reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine dihydrochloride shows anti-proliferative activity to cancer cells
  • 靶点: mAChR1;AChR
  • 体外研究:
    Pirenzepine (100-140 μg/mL; 24 h) inhibits PC-3 cell proliferation activity. Pirenzepine (110 μg/mL; 24 h) inhibits prostate and lung cancer cell migration. Pirenzepine (100-130 μg/mL; 0-24 h) inhibits the expression of GLI1 in PC-3 cells. Cell Proliferation Assay 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 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). Cell Migration Assay Cell Line: PC-3 cells Concentration: 110 μg/mL Incubation Time: 0-24 hours Result: Inhibited the expression of GLI1 and PTCH1. RT-PCR Cell Line: PC-3 cells 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.
  • 体内研究:
    Pirenzepine (intraperitoneal injection; 0.3 mg/kg; once) treatment shows beneficial effects in lipopolysaccharide-induced septic shock. Animal Model: Male C57BL/6 mice with experimental endotoxemia 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.
  • 参考文献:
    1. Carmine AA, et al. Pirenzepine. A review of its pharmacodynamic and pharmacokinetic properties and therapeutic efficacy in peptic ulcer disease and other allied diseases. Drugs. 1985 Aug;30(2):85-126. 2. Yin QQ, et al. Muscarinic acetylcholine receptor M1 mediates prostate cancer cell migration and invasion through hedgehog signaling. Asian J Androl. 2018 Nov-Dec;20(6):608-614. 3. Yabuki Y, et al. The T-type calcium channel enhancer SAK3 inhibits neuronal death following transient brain ischemia via nicotinic acetylcholine receptor stimulation. Neurochem Int. 2017 Sep;108:272-281.
  • 溶解性: Soluble  in  DMSO、H2O
  • 保存条件: 2-8℃
  • 配置溶液浓度参考:
    1mg 5mg 10mg
    1 mM 2.357 ml 11.784 ml 23.567 ml
    5 mM 0.471 ml 2.357 ml 4.713 ml
    10 mM 0.236 ml 1.178 ml 2.357 ml
    50 mM 0.047 ml 0.236 ml 0.471 ml
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