Pirenzepine dihydrochloride

SKU: orb1225401

Description

An antimuscarinic agent that inhibits gastric secretion at lower doses than are required to affect gastrointestinal motility, salivary, central nervous system, cardiovascular, ocular, and urinary function. It promotes the healing of duodenal ulcers and due to its cytoprotective action is beneficial in the prevention of duodenal ulcer recurrence. It also potentiates the effect of other antiulcer agents such as climetidine and panitidine.(In Vitro):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.(In Vivo):Pirenzepine (intraperitoneal injection; 0.3 mg/kg; once) treatment shows beneficial effects in lipopolysaccharide-induced septic shock.

Images & Validation

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Key Properties

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CAS Number	29868-97-1
MW	424.32
Purity	>98% (HPLC)
Formula	C₁₉H₂₁N₅O₂·2HCl
SMILES	Cl.Cl.CN1CCN(CC(=O)N2C3=CC=CC=C3C(=O)NC3=C2N=CC=C3)CC1
Target	AChR
Solubility	Water: 100 mM

Bioactivity

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In Vivo

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.

In Vitro

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.

Storage & Handling

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Storage	Storage temperature: -20°C. Stability: ≥ 2 years
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

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Gene Symbol

AChR

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