Racecadotril (Synonyms: Acetorphan)

Name: Racecadotril
Brand: MedChemExpress
SKU: HY-17399
Rating: 4.5 (1 reviews)

Cat. No.: HY-17399 Purity: 99.83%: FAQs
Data Sheet SDS COA Handling Instructions

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Racecadotril (Acetorphan) is a neutral endopeptidase (NEP) inhibitor. Racecadotril and its active metabolite Thiorphan inhibits purified NEP activity from mouse brain with K_is of 4500 and 6.1 nM, , respectively. Antidiarrheal agent.

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

Racecadotril Chemical Structure

CAS No. : 81110-73-8

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 73	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 73	In-stock	Estimated Time of Arrival: December 31
Solid
200 mg	USD 66	In-stock	Estimated Time of Arrival: December 31
1 g	USD 117	In-stock	Estimated Time of Arrival: December 31
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10 g		Get quote

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Based on 1 publication(s) in Google Scholar

Other Forms of Racecadotril:

Racecadotril-d₅ Get quote
Racecadotril (Standard) Get quote

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References
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Description

Cellular Effect

Cell Line	Type	Value	Description	References
KB 3-1	IC₅₀	2.93 mM Compound: racecadotril	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	[PMID: 21657271]
KB-V1	IC₅₀	1.27 mM Compound: racecadotril	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	[PMID: 21657271]

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].

MedChemExpress (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

Appearance

Solid

Color

White to off-white

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	2 years
	-20°C	1 year

Solvent & Solubility

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.

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

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.

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Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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.

Protocol 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

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 (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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.49 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 99.83%

Select Batch:

Data Sheet (272 KB) SDS (536 KB)

COA (246 KB) LCMS (260 KB)

Handling Instructions (2659 KB)

References

[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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

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

Metabolic Disease

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:

Racecadotril81110-73-8AcetorphanNeprilysinNeutral endopeptidaseNEPCluster of differentiation 10CD10neutralendopeptidaseAntidiarrhealInhibitorinhibitorinhibit

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Racecadotril (Synonyms: Acetorphan)

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Complete Stock Solution Preparation Table

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