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• 產(chǎn)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

• 靶點(diǎn)： mAChR1;AChR

• 體外研究：
  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.

• 體內(nèi)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.

• 參考文獻(xiàn)：
  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

• 保存條件： 2-8℃

• 配置溶液濃度參考：
  

  	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

• 注意：部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶(hù)參考交流研究之用。

輸入產(chǎn)品批號(hào)：

本計(jì)算器可幫助您計(jì)算出特定溶液中溶質(zhì)的質(zhì)量、溶液濃度和體積之間的關(guān)系，公式為：

質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *