Pirenzepine (LS 519) dihydrochloride 是一种选择性的M1 mAChR(毒蕈碱乙酰胆碱受体) 拮抗剂。Pirenzepine dihydrochloride 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 dihydrochloride 具有对癌细胞的抗增殖活性。
| 生物活性 | Pirenzepine (LS 519) dihydrochloride is a selectiveM1mAChR(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 tocancercells[1][2]. |
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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). |
Cell Migration Assay[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 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. |
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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 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: H2O : 75 mg/mL(176.75 mM;Need ultrasonic) DMSO : 25 mg/mL(58.92 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.3567 mL | 11.7836 mL | 23.5671 mL | | 5 mM | 0.4713 mL | 2.3567 mL | 4.7134 mL | | 10 mM | 0.2357 mL | 1.1784 mL | 2.3567 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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