| Size | Price | Stock | Qty |
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| 500mg |
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| 1g |
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| 2g |
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| 5g |
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Purity: ≥98%
Racecadotril (also called acetorphan) is a potent and peripherally acting enkephalinase inhibitor used as an antidiarrheal medication. It has an IC50 of 4.5 μM against enkephalinase and prevents the degradation of endogenous enkephalins. Racecadotril has an antisecretory effect; unlike other opioid medications used to treat diarrhea, it lessens the secretion of water and electrolytes into the intestine while also reducing intestinal motility.
| Targets |
Opioid receptor
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|---|---|
| ln Vivo |
Racecadotril is quickly converted to Thiorphan in mice after intravenous injection; as a result, 30 minutes after the injection, only Thiorphan is found in the kidney and not the parent compound, Racecadotril[1].
In rats, radioactively labeled racecadotril at a single dose of 10 mg/kg is eliminated in 24 hours in 92% of cases[1]. Racecadotril is an inhibitor of neutral endopeptidase (NEP) that has been shown to have antidiarrheal properties in animals. Racecadotril (100 mg/kg) given orally exhibits effectiveness in a rat model of diarrhea brought on by castor oil[2]. |
| Animal Protocol |
6-to-7-week-old male Wistar rats
100 mg/kg A single oral treatment; 30 minutes before castor oil administration. |
| References |
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| Additional Infomation |
2-[[2-[(acetylthio)methyl]-1-oxo-3-phenylpropyl]amino]acetic acid (phenylmethyl) ester is a N-acyl-amino acid.
Racecadotril has been investigated for the basic science and treatment of Diarrhea, Acute Diarrhea, and Acute Gastroenteritis. |
| Molecular Formula |
C21H23NO4S
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| Molecular Weight |
385.48
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| Exact Mass |
385.134
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| Elemental Analysis |
C, 65.43; H, 6.01; N, 3.63; O, 16.60; S, 8.32
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| CAS # |
81110-73-8
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| Related CAS # |
Racecadotril-d5; 1246815-11-1
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| PubChem CID |
107751
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
574.5±50.0 °C at 760 mmHg
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| Melting Point |
89ºC
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| Flash Point |
301.2±30.1 °C
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| Vapour Pressure |
0.0±1.6 mmHg at 25°C
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| Index of Refraction |
1.579
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| LogP |
3.44
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
27
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| Complexity |
485
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(CNC(C(CC1C=CC=CC=1)CSC(C)=O)=O)OCC1C=CC=CC=1
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| InChi Key |
ODUOJXZPIYUATO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H23NO4S/c1-16(23)27-15-19(12-17-8-4-2-5-9-17)21(25)22-13-20(24)26-14-18-10-6-3-7-11-18/h2-11,19H,12-15H2,1H3,(H,22,25)
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| Chemical Name |
benzyl 2-[[2-(acetylsulfanylmethyl)-3-phenylpropanoyl]amino]acetate
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.49 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (6.49 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.49 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5942 mL | 12.9708 mL | 25.9417 mL | |
| 5 mM | 0.5188 mL | 2.5942 mL | 5.1883 mL | |
| 10 mM | 0.2594 mL | 1.2971 mL | 2.5942 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05600062 | Recruiting | Drug: Placebo Drug: Racecadotril 100 milligram (MG) Oral Capsule |
Acute Respiratory Distress Syndrome |
Queen Mary University of London |
August 24, 2023 | Not Applicable |
| NCT01577043 | Completed | Drug: Racecadotril Drug: Placebo |
Acute Diarrhea Acute Gastroenteritis |
Centro Pediatrico Albina de Patino |
September 2011 | Phase 4 |
| NCT05216822 | Completed | Drug: Racecadotril | Acute Watery Diarrhea | Assiut University | June 1, 2018 | Phase 1 |
| NCT01153854 | Completed | Drug: Racecadotril Drug: Placebo groups |
Diarrhea | National Institute of Pediatrics, Mexico |
January 2007 | Phase 3 |
| NCT03473561 | Completed | Drug: Racecadotril plus ORS | Diarrhea, Infantile | Abbott | August 25, 2018 | Phase 3 |
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