Racecadotril
Based on 3 publication(s) in Google Scholar
Racecadotril (Acetorphan) is a neutral endopeptidase (NEP) inhibitor. Racecadotril and its active metabolite Thiorphan inhibits purified NEP activity from mouse brain with Kis of 4500 and 6.1 nM, , respectively. Antidiarrheal agent.
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- Pureté : 99.94%
- CAS No.: 81110-73-8
- Formule: C21H23NO4S
- Masse moléculaire:385.48
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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HY-B0006
Carvedilolβ/α-1 Blocker -
HY-W013375
ThiorphanNEP Inhibitor -
HY-17399R
Racecadotril (Standard)NEP -
HY-15407
SacubitrilNEP Inhibitor -
HY-17620
SacubitrilatNEP Inhibitor -
HY-15407A
Sacubitril hemicalcium saltNEP Inhibitor -
HY-19649
Candoxatril -
HY-15407R
Sacubitril (Standard)NEP Inhibitor -
HY-W345510
OpiorphinhNEP/hAP-N Inhibitor -
HY-18236
MDL-28170Calpain Inhibitor -
HY-14588
LopinavirHIV-1 Protease Inhibitor -
HY-10009
Semagacestatγ-secretase Inhibitor
Publications Citing Use of MedChemExpress (MCE) Racecadotril
More
Activité biologique
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| KB 3-1 | IC50 |
2.93 mM
Compound: racecadotril
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Cytotoxicity against human KB-3-1 cells incubated for 72 hrs by MTT assay
Cytotoxicity against human KB-3-1 cells incubated for 72 hrs by MTT assay
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[PMID: 21657271] |
| KB-V1 | IC50 |
1.27 mM
Compound: racecadotril
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Cytotoxicity against drug-resistant human KBV1 cells expressing P-gp incubated for 72 hrs by MTT assay
Cytotoxicity against drug-resistant human KBV1 cells expressing P-gp incubated for 72 hrs by MTT assay
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[PMID: 21657271] |
In Vivo
In rats 92% of a single-dose (10 mg/kg) of radioactively labeled Racecadotril is eliminated within 24 h[1].
Racecadotril is a neutral endopeptidase (NEP) inhibitor with known antidiarrheal activity in animals. Orally administered Racecadotril (100 mg/kg ) shows efficacy in a rat model of castor oil-induced diarrhea[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:6-to-7-week-old male Wistar rats[2]
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Dosage:100 mg/kg
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Administration:A single oral treatment; 30 minutes before castor oil administration.
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Result:Significantly reduced stool output but did not prevent the occurrence of diarrhea (100% incidence).
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 81110-73-8
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Appearance Solid
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Masse moléculaire 385.48
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Formule C21H23NO4S
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Color White to off-white
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SMILES
O=C(OCC1=CC=CC=C1)CNC(C(CSC(C)=O)CC2=CC=CC=C2)=O
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Synonyms
Acetorphan
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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ACS Environ Au
Machine Learning-Assisted Recognition of Environmental Sulfur-Containing Chemicals in Nontargeted Mass Spectrometry Analysis of Inadequate Mass Resolution. [Abstract]2025 Aug 5;5(6):573-582. PMID: 41277996 -
Anal Chem
Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]2025 Jun 3;97(21):11099-11109. PMID: 40401576 -
Neuropharmacology
Pharmacological and electrophysiological characterization of the novel Kv7 channel inhibitor racecadotril in Parkinson's disease. [Abstract]2025 Nov 1:278:110565. PMID: 40532787
Solvant et solubilité
In Vitro:
DMSO : ≥ 100 mg/mL (259.42 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.49 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (6.49 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureté et documentation
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Fiche technique (273 KB)
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SDS (597 KB)
- English - EN (597 KB)
- Français - FR (597 KB)
- Deutsch - DE (597 KB)
- Norwegian - NO (597 KB)
- Español - ES (597 KB)
- Swedish - SV (597 KB)
- Italian - IT (597 KB)
- Korean - KR (597 KB)
- Portuguese - PT (597 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Marion Eberlin, et al. A comprehensive review of the pharmacodynamics, pharmacokinetics, and clinical effects of the neutral endopeptidase inhibitor Racecadotril. Front Pharmacol. 2012 May 30;3:93. [Content Brief]
[2]. David W Griggs, et al. Pharmacologic Comparison of Clinical Neutral Endopeptidase Inhibitors in a Rat Model of Acute Secretory Diarrhea. J Pharmacol Exp Ther. 2016 May;357(2):423-31. [Content Brief]
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 |
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| DMSO | 1 mM | 2.5942 mL | 12.9708 mL | 25.9417 mL | 64.8542 mL |
| 5 mM | 0.5188 mL | 2.5942 mL | 5.1883 mL | 12.9708 mL | |
| 10 mM | 0.2594 mL | 1.2971 mL | 2.5942 mL | 6.4854 mL | |
| 15 mM | 0.1729 mL | 0.8647 mL | 1.7294 mL | 4.3236 mL | |
| 20 mM | 0.1297 mL | 0.6485 mL | 1.2971 mL | 3.2427 mL | |
| 25 mM | 0.1038 mL | 0.5188 mL | 1.0377 mL | 2.5942 mL | |
| 30 mM | 0.0865 mL | 0.4324 mL | 0.8647 mL | 2.1618 mL | |
| 40 mM | 0.0649 mL | 0.3243 mL | 0.6485 mL | 1.6214 mL | |
| 50 mM | 0.0519 mL | 0.2594 mL | 0.5188 mL | 1.2971 mL | |
| 60 mM | 0.0432 mL | 0.2162 mL | 0.4324 mL | 1.0809 mL | |
| 80 mM | 0.0324 mL | 0.1621 mL | 0.3243 mL | 0.8107 mL | |
| 100 mM | 0.0259 mL | 0.1297 mL | 0.2594 mL | 0.6485 mL |
Racecadotril Related Classifications
HY-17399 Related Classifications
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