2. GPCR/G Protein Neuronal Signaling Apoptosis Autophagy
  3. 5-HT Receptor Apoptosis Autophagy
  4. Prucalopride

Prucalopride is an orally active, selective and specific 5-HT 4 receptor agonist (high affinity), with pKis of 8.6 and 8.1 for human 5-HT4a/4b receptors, respectively. Prucalopride improves intestinal motility by promoting regeneration of the intestinal nervous system in rats. Prucalopride also shows anticancer activity by blocking of the PI3K/AKT/mTor signaling pathway. Prucalopride can be used in studies of chronic constipation, pseudo-intestinal obstruction and cancer.

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Prucalopride Chemical Structure

Prucalopride Chemical Structure

CAS No. : 179474-81-8

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 37 In-stock
Solution
10 mM * 1 mL in DMSO USD 37 In-stock
Solid
5 mg USD 34 In-stock
10 mg USD 48 In-stock
50 mg USD 85 In-stock
100 mg USD 140 In-stock
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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of Prucalopride:

Prucalopride Related Antibodies

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5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor 5-HT Receptor

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Prucalopride is an orally active, selective and specific 5-HT 4 receptor agonist (high affinity), with pKis of 8.6 and 8.1 for human 5-HT4a/4b receptors, respectively. Prucalopride improves intestinal motility by promoting regeneration of the intestinal nervous system in rats. Prucalopride also shows anticancer activity by blocking of the PI3K/AKT/mTor signaling pathway. Prucalopride can be used in studies of chronic constipation, pseudo-intestinal obstruction and cancer[1][2][3].

IC50 & Target

5-HT4A Receptor

8.6 (pKi)

5-HT4B Receptor

8.1 (pKi)

In Vitro

Prucalopride (10 μM; 24, 48, 72 h) shows anti proliferative activity in A549 cells[1].
Prucalopride induces autophagy and apoptosis, decreases the expression of the phosphorylated protein kinase B (AKT) and mammalian target of rapamycin (mTor) in A549/A427 cells[1].

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

Prucalopride Related Antibodies

Cell Proliferation Assay[1]

Cell Line: A549 cells
Concentration: 10 µM
Incubation Time: 24, 48, 72 h
Result: Repressed lung cancer cells proliferation.
In Vivo

Prucalopride (5, 10 μg/kg; p.o.; single daily for 2 weeks) shortens the colonic transit time in DM model, promotes the regeneration of colonic neural stem cells and neurons[2].
Prucalopride (5, 10 μg/kg; p.o.; single daily for 2 weeks) promotes the differentiation of colonic neural stem cells, activates the expression of glial proteins and promotes the recovery of neuronal injury to a certain extent[2].

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

Animal Model: Sprague dawley rats (diabetes mellitus (DM) model)[2].
Dosage: 5 or 10 µg/kg
Administration: Oral gavage; single daily for 2 weeks.
Result: Accelerated colonic movement and shortened the colonic transit time, and markedly increased the expression levels of Ki67.
Increased expression of SOX10 in the columnar epithelial nuclei and enteraden (when at 5 µg/kg), and in the columnar epithelial cells, the nuclei of lamina propria cells and enteraden (when at 10 µg/kg).
Significantly increased Nestin expression, which concentrated in columnar epithelial cells and the mesenchyme. (Nestin:a marker of enteric neural stem cells in the ENS).
Clinical Trial
Molecular Weight

367.87

Formula

C18H26ClN3O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

ClC1=C(N)C(CCO2)=C2C(C(NC3CCN(CCCOC)CC3)=O)=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

H2O : 50 mg/mL (135.92 mM; Need ultrasonic)

DMSO : ≥ 31 mg/mL (84.27 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7184 mL 13.5918 mL 27.1835 mL
5 mM 0.5437 mL 2.7184 mL 5.4367 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* 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
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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

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Volume (final)

V2

In Vivo:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  PBS

    Solubility: 50 mg/mL (135.92 mM); Clear solution; Need ultrasonic

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

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 1 mM 2.7184 mL 13.5918 mL 27.1835 mL 67.9588 mL
5 mM 0.5437 mL 2.7184 mL 5.4367 mL 13.5918 mL
10 mM 0.2718 mL 1.3592 mL 2.7184 mL 6.7959 mL
15 mM 0.1812 mL 0.9061 mL 1.8122 mL 4.5306 mL
20 mM 0.1359 mL 0.6796 mL 1.3592 mL 3.3979 mL
25 mM 0.1087 mL 0.5437 mL 1.0873 mL 2.7184 mL
30 mM 0.0906 mL 0.4531 mL 0.9061 mL 2.2653 mL
40 mM 0.0680 mL 0.3398 mL 0.6796 mL 1.6990 mL
50 mM 0.0544 mL 0.2718 mL 0.5437 mL 1.3592 mL
60 mM 0.0453 mL 0.2265 mL 0.4531 mL 1.1326 mL
80 mM 0.0340 mL 0.1699 mL 0.3398 mL 0.8495 mL
H2O 100 mM 0.0272 mL 0.1359 mL 0.2718 mL 0.6796 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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Prucalopride 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:

Prucalopride179474-81-85-HT ReceptorApoptosisAutophagySerotonin Receptor5-hydroxytryptamine ReceptorLung cancerchronic constipationpseudo-intestinal obstructionA549A427Inhibitorinhibitorinhibit

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