| 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，僅供客戶參考交流研究之用。 |
上海工商
危險(xiǎn)品化學(xué)品經(jīng)營(yíng)許可證（不帶存儲(chǔ)）
營(yíng)業(yè)執(zhí)照(三證合一)
北京