Pirenzepine (LS 519 free base) 是一种选择性的M1 mAChR(毒蕈碱乙酰胆碱受体) 拮抗剂。Pirenzepine 可减少胃酸分泌并减少肌肉痉挛，可用于消化性溃疡的研究。Pirenzepine 具有对癌细胞的抗增殖活性。
| 生物活性 | Pirenzepine (LS 519 free base) is a selectiveM1mAChR(muscarinic acetylcholine receptor) antagonist. Pirenzepine reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine shows anti-proliferative activity tocancercells[1][2]. |
体外研究
(In Vitro) | 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. |
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体内研究
(In Vivo) | 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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