Art. -Nr.: HY-17037A

Pirenzepine

(Synonyms: LS 519 free base; Pirenzepin; Gastrozepin)

5 Cited Publications

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Based on 5 publication(s) in Google Scholar

Pirenzepine (LS 519 free base) is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist, with poor penetration of the blood-brain barrier. Pirenzepine reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine shows anti-proliferative activity to cancer cells.

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Reinheit: 99.13%
CAS. Nr.: 28797-61-7
Formel: C₁₉H₂₁N₅O₂
Molecular Weight:351.40

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Pirenzepine Chemical Structure

CAS. Nr.: 28797-61-7

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Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (5)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle mAChR Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	119 nM Compound: pirenzepine	Compound was tested for its binding affinity against M1 human recombinant muscarinic receptor in CHO cells. Compound was tested for its binding affinity against M1 human recombinant muscarinic receptor in CHO cells.	[PMID: 10522693]
CHO	IC₅₀	2.1 x 10^-8 M Compound: Pirenzepine	Displacement of [3H]pirenzepine from human recombinant muscarinic M1 receptor expressed in CHO cells Displacement of [3H]pirenzepine from human recombinant muscarinic M1 receptor expressed in CHO cells	[PMID: 26988801]
CHO	IC₅₀	2.1 x 10^-8 M Compound: Pirenzepine	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	[PMID: 27876250]
CHO	IC₅₀	246.8 nM Compound: pirenzepine	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	[PMID: 9986705]
CHO	IC₅₀	28.2 nM Compound: pirenzepine	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	[PMID: 9986705]
CHO	IC₅₀	340.6 nM Compound: pirenzepine	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	[PMID: 9986705]
CHO	IC₅₀	955.6 nM Compound: pirenzepine	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	[PMID: 9986705]
CHO	IC₅₀	968.2 nM Compound: pirenzepine	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	[PMID: 9986705]

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.

In Vivo

Pirenzepine (intraperitoneal injection; 0.3 mg/kg; once) treatment shows beneficial effects in lipopolysaccharide-induced septic shock^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Chemical Information

CAS. Nr. 28797-61-7
Appearance Solid
Molecular Weight 351.40
Formel C₁₉H₂₁N₅O₂
Color Light yellow to yellow
SMILES

O=C1NC2=CC=CN=C2N(C(CN3CCN(C)CC3)=O)C4=CC=CC=C14
Synonyms

LS 519 free base; Pirenzepin; Gastrozepin
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (5)

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Journal Impact Factor

Cell Rep

Carvedilol sensitizes chemotherapy by targeting STING to boost anti-tumor immunity. [Abstract]

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 Jan 21:599:112464. PMID: 39848433
Research Square Preprint

2021 Jan.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (284.58 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.8458 mL

14.2288 mL

28.4576 mL

5 mM

0.5692 mL

2.8458 mL

5.6915 mL

10 mM

0.2846 mL

1.4229 mL

2.8458 mL

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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 5 mg/mL (14.23 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 5 mg/mL (14.23 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. 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
DMSO	1 mM	2.8458 mL	14.2288 mL	28.4576 mL	71.1440 mL
	5 mM	0.5692 mL	2.8458 mL	5.6915 mL	14.2288 mL
	10 mM	0.2846 mL	1.4229 mL	2.8458 mL	7.1144 mL
	15 mM	0.1897 mL	0.9486 mL	1.8972 mL	4.7429 mL
	20 mM	0.1423 mL	0.7114 mL	1.4229 mL	3.5572 mL
	25 mM	0.1138 mL	0.5692 mL	1.1383 mL	2.8458 mL
	30 mM	0.0949 mL	0.4743 mL	0.9486 mL	2.3715 mL
	40 mM	0.0711 mL	0.3557 mL	0.7114 mL	1.7786 mL
	50 mM	0.0569 mL	0.2846 mL	0.5692 mL	1.4229 mL
	60 mM	0.0474 mL	0.2371 mL	0.4743 mL	1.1857 mL
	80 mM	0.0356 mL	0.1779 mL	0.3557 mL	0.8893 mL
	100 mM	0.0285 mL	0.1423 mL	0.2846 mL	0.7114 mL

Keywords

Pirenzepine

5 Cited Publications

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Pirenzepine

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Publications Citing Use of MedChemExpress (MCE) Pirenzepine

Alle mAChR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (5)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Pirenzepine

GPCR/G Protein Compound Library

Neuronal Signaling Compound Library

FDA-Approved Drug Library

Anti-Cancer Compound Library

Drug Repurposing Compound Library

Neurotransmitter Receptor Compound Library

FDA Approved & Pharmacopeial Drug Library

Anti-Lung Cancer Compound Library

Anti-Parkinson's Disease Compound Library

Neurodegenerative Disease-related Compound Library

FDA-Approved Anticancer Drug Library

Human Metabolite Library

Heterocyclic Compound Library

Off-patent Drug Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Chinese Baijiu Compound Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) Pirenzepine

Alle mAChR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (5)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Pirenzepine Related Classifications

HY-17037A Related Classifications