Pirenzepine dihydrochloride
Based on 5 publication(s) in Google Scholar
Pirenzepine (LS 519) dihydrochloride is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist, with poor penetration of the blood-brain barrier. 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.
For research use only. We do not sell to patients.
- Purity: 99.84%
- CAS No.: 29868-97-1
- Formula: C19H23Cl2N5O2
- Molecular Weight:424.32
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Pirenzepine dihydrochloride
More
Biological Activity
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mAChR1 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
2.1 x 10-2μM
Compound: Pirenzepine
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Displacement of [3H]pirenzepine from human recombinant M1 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
Displacement of [3H]pirenzepine from human recombinant M1 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
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[PMID: 27876250] |
| CHO | IC50 |
246.8 nM
Compound: pirenzepine
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Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
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[PMID: 9986705] |
| CHO | IC50 |
28.2 nM
Compound: pirenzepine
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Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M1 using membranes from transfected CHO cells
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M1 using membranes from transfected CHO cells
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[PMID: 9986705] |
| CHO | IC50 |
340.6 nM
Compound: pirenzepine
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Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M5 using membranes from transfected CHO cells
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M5 using membranes from transfected CHO cells
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[PMID: 9986705] |
| CHO | IC50 |
955.6 nM
Compound: pirenzepine
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Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
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[PMID: 9986705] |
| CHO | IC50 |
968.2 nM
Compound: pirenzepine
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Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M2 using membranes from transfected CHO cells
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M2 using membranes from transfected CHO cells
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[PMID: 9986705] |
Pirenzepine (100-140 μg/mL; 24 h) dihydrochloride inhibits PC-3 cell proliferation activity[2].
Pirenzepine (110 μg/mL; 24 h) dihydrochloride inhibits prostate and lung cancer cell migration[2].
Pirenzepine (100-130 μg/mL; 0-24 h) dihydrochloride inhibits the expression of GLI1 in PC-3 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PC-3 cells
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Concentration:100-140 μg/mL
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Incubation Time:24 hours
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Result:Inhibited PC-3 cell proliferation in a concentration-dependent manner.
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Cell Line:PC-3 and A549 cells
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Concentration:110 μg/mL
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Incubation Time:24 hours
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Result:Inhibited the migration of PC-3 and A549 cell lines (P=0.014).
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Cell Line:PC-3 cells
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Concentration:110 μg/mL
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Incubation Time:0-24 hours
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Result:Inhibited the expression of GLI1 and PTCH1.
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Cell Line:PC-3 cells
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Concentration:100-130 μg/mL
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Incubation Time:24 hours
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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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6 mice with experimental endotoxemia[3]
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Dosage:0.3 mg/kg
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Administration:Intraperitoneal injection; 0.3 mg/kg; once
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Result:Improved survival rate of LPS-induced septic shock.
Relieved LPS-induced pulmonary and hepatic injury.
Reduced the expression of SOCS3 at mRNA level.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 29868-97-1
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Appearance Solid
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Molecular Weight 424.32
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Formula C19H23Cl2N5O2
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Color White to yellow
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SMILES
O=C1NC2=CC=CN=C2N(C(CN3CCN(C)CC3)=O)C4=CC=CC=C14.[H]Cl.[H]Cl
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Synonyms
LS 519; Pirenzepin dihydrochloride; Gastrozepin dihydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (5)
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Journal Impact Factor
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Most Recent
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Cell Rep
2025 Apr 16;44(5):115572. PMID: 40249703 -
Eur J Med Res
Pirenzepine exhibits anti-prostate cancer activity and enhances checkpoint inhibitor-based immunotherapy by targeting STING. [Abstract]2025 Dec 23;30(1):1250. PMID: 41430631 -
Ther Adv Med Oncol
Repurposing of ivacaftor shows potential to treat ROR1 expressing high-grade serous ovarian cancer. [Abstract]2026 Jan 2:18:17588359251409010. PMID: 41487693 -
Mol Cell Endocrinol
Vagotomy suppresses food intake by increasing GLP-1 secretion via the M3 AChR-AMPKα pathway in mice. [Abstract]2025 Apr 1:599:112464. PMID: 39848433 -
Solvent & Solubility
H2O : 50 mg/mL (117.84 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (283 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 2.3567 mL | 11.7836 mL | 23.5671 mL | 58.9178 mL |
| 5 mM | 0.4713 mL | 2.3567 mL | 4.7134 mL | 11.7836 mL | |
| 10 mM | 0.2357 mL | 1.1784 mL | 2.3567 mL | 5.8918 mL | |
| 15 mM | 0.1571 mL | 0.7856 mL | 1.5711 mL | 3.9279 mL | |
| 20 mM | 0.1178 mL | 0.5892 mL | 1.1784 mL | 2.9459 mL | |
| 25 mM | 0.0943 mL | 0.4713 mL | 0.9427 mL | 2.3567 mL | |
| 30 mM | 0.0786 mL | 0.3928 mL | 0.7856 mL | 1.9639 mL | |
| 40 mM | 0.0589 mL | 0.2946 mL | 0.5892 mL | 1.4729 mL | |
| 50 mM | 0.0471 mL | 0.2357 mL | 0.4713 mL | 1.1784 mL | |
| 60 mM | 0.0393 mL | 0.1964 mL | 0.3928 mL | 0.9820 mL | |
| 80 mM | 0.0295 mL | 0.1473 mL | 0.2946 mL | 0.7365 mL | |
| 100 mM | 0.0236 mL | 0.1178 mL | 0.2357 mL | 0.5892 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Pirenzepine dihydrochloride Related Classifications
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