S84820 |
Pirenzepine dihydrochloride |
| MedMol | 99% |
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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
- 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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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)
