1. Metabolic Enzyme/Protease
  2. Neprilysin
  3. Racecadotril

Racecadotril (Synonyms: Acetorphan)

Cat. No.: HY-17399 Purity: 98.85%
Handling Instructions

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.

For research use only. We do not sell to patients.

Racecadotril Chemical Structure

Racecadotril Chemical Structure

CAS No. : 81110-73-8

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10 mM * 1 mL in DMSO USD 66 In-stock
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Description

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[1].

In Vivo

In mice, following i.v. administration, Racecadotril is rapidly metabolized to Thiorphan; thus, 30 min after the injection only Thiorphan is recovered from the kidney whereas the parent compound Racecadotril is not detected[1].
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].

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

Animal Model: 6-to-7-week-old male Wistar rats[2]
Dosage: 100 mg/kg
Administration: A single oral treatment; 30 minutes before castor oil administration.
Result: Significantly reduced stool output but did not prevent the occurrence of diarrhea (100% incidence).
Clinical Trial
Molecular Weight

385.48

Formula

C₂₁H₂₃NO₄S

CAS No.

81110-73-8

SMILES

O=C(OCC1=CC=CC=C1)CNC(C(CSC(C)=O)CC2=CC=CC=C2)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (259.42 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    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

  • 2.

    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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.49 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

RacecadotrilAcetorphanNeprilysinNeutral endopeptidaseNEPCluster of differentiation 10CD10neutralendopeptidaseAntidiarrhealInhibitorinhibitorinhibit

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Product Name:
Racecadotril
Cat. No.:
HY-17399
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