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

Pirenzepine dihydrochloride  (Synonyms: LS 519; Pirenzepin dihydrochloride; Gastrozepin dihydrochloride)

Cat. No.: HY-17037 Purity: 99.89%
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Pirenzepine (LS 519) dihydrochloride is a selective M1 mAChR (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 to cancer cells.

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

Pirenzepine dihydrochloride Chemical Structure

Pirenzepine dihydrochloride Chemical Structure

CAS No. : 29868-97-1

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 44 In-stock
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500 mg USD 90 In-stock
1 g USD 162 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Pirenzepine dihydrochloride:

Pirenzepine dihydrochloride Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Pirenzepine dihydrochloride

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) dihydrochloride is a selective M1 mAChR (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 to cancer cells[1][2].

IC50 & Target

mAChR1

 

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 dihydrochloride 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).

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.
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

424.32

Formula

C19H23Cl2N5O2
CAS No.
Appearance

Solid

Color

White to yellow

SMILES

O=C1NC2=CC=CN=C2N(C(CN3CCN(C)CC3)=O)C4=CC=CC=C14.[H]Cl.[H]Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

H2O : 50 mg/mL (117.84 mM; Need ultrasonic)

DMSO : 25 mg/mL (58.92 mM; Need ultrasonic; 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 2.3567 mL 11.7836 mL 23.5671 mL
5 mM 0.4713 mL 2.3567 mL 4.7134 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 (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.

  • Molarity Calculator

  • Dilution Calculator

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 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.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
Purity & Documentation

Purity: 99.89%

COA (256 KB) LCMS (96 KB)

Handling Instructions (2659 KB)
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 (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
DMSO / 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
H2O 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.

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Pirenzepine dihydrochloride 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:

Pirenzepine29868-97-1LS 519PirenzepinGastrozepinLS519LS-519mAChRMuscarinic acetylcholine receptorpeptic ulcersanti-proliferative activityPC-3A549Inhibitorinhibitorinhibit

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