2. GPCR/G Protein Neuronal Signaling
  3. mAChR
  4. Pirenzepine

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

Cat. No.: HY-17037A Purity: 98.84%
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Pirenzepine (LS 519 free base) is a selective M1 mAChR (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 to cancer cells.

For research use only. We do not sell to patients.

Pirenzepine Chemical Structure

Pirenzepine Chemical Structure

CAS No. : 28797-61-7

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Based on 1 publication(s) in Google Scholar

Other Forms of Pirenzepine:

Pirenzepine Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Pirenzepine

View All mAChR Isoform Specific Products:

View All Isoforms
mAChR1 mAChR2 mAChR3 mAChR4 mAChR5

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Pirenzepine (LS 519 free base) is a selective M1 mAChR (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 to cancer cells[1][2].

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.

Pirenzepine Related Antibodies

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.
Molecular Weight

351.40

Formula

C19H21N5O2
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8458 mL 14.2288 mL 28.4576 mL
5 mM 0.5692 mL 2.8458 mL 5.6915 mL
View the 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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

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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

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. 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
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Pirenzepine Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Pirenzepine28797-61-7LS 519 Pirenzepin GastrozepinLS519LS-519mAChRMuscarinic acetylcholine receptorpeptic ulcersanti-proliferative activityPC-3A549Inhibitorinhibitorinhibit

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