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> Pirenzepine (dihydrochloride) [29868-97-1]

Pirenzepine (dihydrochloride) [29868-97-1]

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Cat# HY-17037-100mg

Size : 100mg

Brand : MedChemExpress

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Description

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[1][2].

IC50 & Target

mAChR1

 

Cellular Effect
Cell Line Type Value Description References
CHO IC50
2.1 x 10-2μM
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) 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.

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) dihydrochloride 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.
Clinical Trial
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=C14.01Cl.01Cl
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)

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)

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

This equation is commonly abbreviated as: C1V1 = C2V2

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
References

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