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

Prucalopride succinate  (Synonyms: R-108512)

Cat. No.: HY-12694 Purity: 99.95%
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Prucalopride succinate 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 succinate improves intestinal motility by promoting regeneration of the intestinal nervous system in rats. Prucalopride succinate also shows anticancer activity by blocking of the PI3K/AKT/mTor signaling pathway. Prucalopride succinate can be used in studies of chronic constipation, pseudo-intestinal obstruction and cancer.

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Prucalopride succinate Chemical Structure

Prucalopride succinate Chemical Structure

CAS No. : 179474-85-2

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Based on 2 publication(s) in Google Scholar

Other Forms of Prucalopride succinate:

Prucalopride succinate Related Antibodies

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Description

Prucalopride succinate 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 succinate improves intestinal motility by promoting regeneration of the intestinal nervous system in rats. Prucalopride succinate also shows anticancer activity by blocking of the PI3K/AKT/mTor signaling pathway. Prucalopride succinate can be used in studies of chronic constipation, pseudo-intestinal obstruction and cancer[1][2][3][4].

IC50 & Target

5-HT4A Receptor

8.6 (pKi)

5-HT4B Receptor

8.1 (pKi)

In Vitro

Prucalopride succinate (10 µM; 24, 48, 72 h) shows anti proliferative activity in A549 cells[4].
Prucalopride succinate induces autophagy and apoptosis, decreases the expression of the phosphorylated protein kinase B (AKT) and mammalian target of rapamycin (mTor) in A549/A427 cells[4].

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

Prucalopride succinate Related Antibodies

Cell Proliferation Assay

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

Prucalopride succinate (5 mg/kg, s.c) increases ACh and histamine levels in the rat prefrontal cortex[2].
Prucalopride succinate (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[3].
Prucalopride succinate (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[3].

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

Animal Model: Diabetes mellitus (DM) rat models[3]
Dosage: 5 μg/kg, 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

485.96

Formula

C22H32ClN3O7
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(O)CCC(O)=O.O=C(C1=C(OCC2)C2=C(N)C(Cl)=C1)NC3CCN(CCCOC)CC3
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: 

DMSO : 50 mg/mL (102.89 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : ≥ 20 mg/mL (41.16 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0578 mL 10.2889 mL 20.5778 mL
5 mM 0.4116 mL 2.0578 mL 4.1156 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)

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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: ≥ 2.5 mg/mL (5.14 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (5.14 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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:

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(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: 99.95%

SDS (393 KB)

COA (250 KB) HNMR (286 KB) LCMS (94 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
H2O / DMSO 1 mM 2.0578 mL 10.2889 mL 20.5778 mL 51.4446 mL
5 mM 0.4116 mL 2.0578 mL 4.1156 mL 10.2889 mL
10 mM 0.2058 mL 1.0289 mL 2.0578 mL 5.1445 mL
15 mM 0.1372 mL 0.6859 mL 1.3719 mL 3.4296 mL
20 mM 0.1029 mL 0.5144 mL 1.0289 mL 2.5722 mL
25 mM 0.0823 mL 0.4116 mL 0.8231 mL 2.0578 mL
30 mM 0.0686 mL 0.3430 mL 0.6859 mL 1.7148 mL
40 mM 0.0514 mL 0.2572 mL 0.5144 mL 1.2861 mL
DMSO 50 mM 0.0412 mL 0.2058 mL 0.4116 mL 1.0289 mL
60 mM 0.0343 mL 0.1715 mL 0.3430 mL 0.8574 mL
80 mM 0.0257 mL 0.1286 mL 0.2572 mL 0.6431 mL
100 mM 0.0206 mL 0.1029 mL 0.2058 mL 0.5144 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 succinate 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:

Prucalopride179474-85-2R-108512R108512R 1085125-HT ReceptorApoptosisAutophagySerotonin Receptor5-hydroxytryptamine Receptor5-HT4AgonistAChHistamineA547DM rat modelInhibitorinhibitorinhibit

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