Domperidone (R33812)

Alias: KW 5338; Domperidone; KW5338; KW-5338; Motilium; Domperidona

Cat No.:V1262 Purity: ≥98%

COA Product Data Instructions for use SDS

Domperidone (R 33812; R-33812; KW5338; KW-5338; Motilium; Domperidona) is an orally bioactive dopamine D2 receptor antagonist and an antiemetic medication used to relieve nausea and vomiting.

Domperidone (R33812) Chemical Structure CAS No.: 57808-66-9
Product category: Dopamine Receptor

This product is for research use only, not for human use. We do not sell to patients.

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Top Publications Citing lnvivochem Products

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J Am Chem Soc 2022,144:21831-21836.

Cell 2020,183:1202-1218.e25.

Science Adv 2022:8,eabm9427.

Nature 2021,597(7874):119-125.

Cell 2020,183:1202-1218.e25.

PNAS Nexus 2022,1(3):pgac063.

ACS Nano 2023,17(10):9110-9125.

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Purity & Quality Control Documentation

Current batch：

Purity: ≥98%

COA

MSDS

NMR

Instructions

Product Description
Bioactivity & Protocols
Physicochemical Properties
Solubility Data
Calculators
Clinical Trial Information
Biological Data

Product Description

Domperidone (R 33812; R-33812; KW5338; KW-5338; Motilium; Domperidona) is an orally bioactive dopamine D2 receptor antagonist and an antiemetic medication used to relieve nausea and vomiting. It also functions as a galactagogue and a gastric prokinetic agent. Because it is more tolerable than metoclopramide, domperidone is a good substitute for it in the treatment of gastroparesis. In Madin-Darby bovine kidney (MDBK) cells, the D2R antagonist domeperidone inhibits Equilibrative NT1 (ENT1) activity more when bromocriptine is present than when it is not, and it has a lower IC50 value than both of these drugs.

Biological Activity I Assay Protocols (From Reference)

Targets

Dopamine D2 receptor

ln Vitro

In vitro activity: Domperidone (a D2R antagonist) inhibits Equilibrative NT1 (ENT1) activity more when bromocriptine is present than when it is not, and it has a lower IC50 value than both of these drugs in Madin-Darby bovine kidney (MDBK) cells.[1]

ln Vivo

Domperidone (0.1 mg/kg) significantly reduces feeding behavior and increases basal metabolism, but it has no effect on locomotor activity in ats housed in a Phenomaster system.[2] Domperidone (1.1 mg/kg and 5.5 mg/kg, oral) dramatically raises laminar microvascular blood flow (LMBF) in horses starting 4 hours after administration and keeps the effect going for at least 8 hours. This is in comparison with baseline values. When administered intravenously at a dose of 0.2 mg/kg, doperidone dramatically raises laminar microvascular blood flow (LMBF) in horses at 10 and 12 hours after baseline.[3] Domperidone can lessen the negative effects on reproduction and decrease weight gain in heifers affected by fescue toxicosis. [4] Compared to control mares, mares treated with domeperidone had shorter gestations and foaled closer to their anticipated parturition date. Mares receiving dopamine treatment have greater serum prolactin concentrations and Mammary gland scores. [5] In rats, dopamine (5 mg/kg, oral) increases the area under the curve and peak plasma acetaminophen concentration, suggesting enhanced gastric emptying. Domperidone reduces the rat midjejunal longitudinal muscle strips' dopamine-induced contractile activity.[6]

Animal Protocol

1.1 mg/kg and 5.5 mg/kg, oral

Rats

References

[1]. J Agric Food Chem . 2011 Sep 14;59(17):9691-9

[2]. Bull Exp Biol Med . 2013 Oct;155(6):705-7.

[3]. Am J Vet Res . 2010 Mar;71(3):281-7.

[4]. J Anim Sci . 2003 Oct;81(10):2568-74.

[5]. Am J Vet Res . 1994 May;55(5):722-9.

[6]. Am J Vet Res . 2013 Aug;74(8):1103-10.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Physicochemical Properties

Molecular Formula

C22H24CLN5O2

Molecular Weight

425.91

Exact Mass

425.16

Elemental Analysis

C, 62.04; H, 5.68; Cl, 8.32; N, 16.44; O, 7.51

CAS #

57808-66-9

Related CAS #

Domperidone monomaleate; 83898-65-1; Domperidone-d6; 1329614-18-7

Appearance

Solid powder

SMILES

C1CN(CCC1N2C3=C(C=C(C=C3)Cl)NC2=O)CCCN4C5=CC=CC=C5NC4=O

InChi Key

FGXWKSZFVQUSTL-UHFFFAOYSA-N

InChi Code

InChI=1S/C22H24ClN5O2/c23-15-6-7-20-18(14-15)25-22(30)28(20)16-8-12-26(13-9-16)10-3-11-27-19-5-2-1-4-17(19)24-21(27)29/h1-2,4-7,14,16H,3,8-13H2,(H,24,29)(H,25,30)

Chemical Name

6-chloro-3-[1-[3-(2-oxo-3H-benzimidazol-1-yl)propyl]piperidin-4-yl]-1H-benzimidazol-2-one

Synonyms

KW 5338; Domperidone; KW5338; KW-5338; Motilium; Domperidona

HS Tariff Code

2934.99.9001

Storage

Powder -20°C 3 years

4°C 2 years

In solvent -80°C 6 months

-20°C 1 month

Shipping Condition

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Solubility Data

Solubility (In Vitro)

DMSO: 48~50 mg/mL (112.7~117.4 mM)

Water: <1 mg/mL

Ethanol: <1 mg/mL

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.75 mg/mL (6.46 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 27.5 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: ≥ 2.75 mg/mL (6.46 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 27.5 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.

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Solubility in Formulation 3: ≥ 2.75 mg/mL (6.46 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 27.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

(Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.3479 mL	11.7396 mL	23.4791 mL
	5 mM	0.4696 mL	2.3479 mL	4.6958 mL
	10 mM	0.2348 mL	1.1740 mL	2.3479 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.

Calculator

Mass

Concentration

Volume

Molecular Weight*

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Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

Calculate the Mass of a compound required to prepare a solution of known volume and concentration
Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?

Enter 350.26 in the Molecular Weight (MW) box
Enter 10 in the Concentration box and choose the correct unit (mM)
Enter 5 in the Volume box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

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Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:

Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
Enter 25 into the Concentration (End) box and select the correct unit (mM)
Enter 25 into the Volume (End) box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box

Molecular formula

Total molecular weight

g/mol

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Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4 c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
Click the “Calculate” button
The answer appears in the Volume (to add to vial) box

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)

Dosage mg/kg

Average weight of animals g

Dosing volume per animal μL

Number of animals

Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)

% DMSO

% Tween 80

% ddH₂O

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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.

Note： (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.

Clinical Trial Information

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT06171087	Recruiting	Drug: Domperidon Drug: Placebo	Emotions	German Institute of Human Nutrition	August 1, 2023	Phase 4
NCT01696734	Recruiting	Drug: Domperidone Other: Questionnaire Administration	Dyspepsia Esophagitis Gastroparesis	M.D. Anderson Cancer Center	October 23, 2012	Phase 3
NCT04699591	Recruiting	Drug: Domperidone	GERD Gastroparesis Gastroesophageal Reflux	Children's Mercy Hospital Kansas City	April 2013	Not Applicable
NCT03221855	Completed	Drug: Placebo Drug: Domperidone	Breastfeeding	Hospital de Clinicas de Porto Alegre	March 2013	Early Phase 1
NCT03617016	Completed	Drug: Placebo Drug: Domperidone	Dyspepsia	Xian-Janssen Pharmaceutical Ltd.	August 27, 2018	Phase 4

Biological Data

Mean ± SD plasma acetaminophen concentration determined during an acetaminophen absorption test in 2 groups of 6 horses that were administered domperidone paste (1.1 [A] or 5.0 mg [B] of domperidone/kg; circles) or placebo paste (rectangles) orally (2 treatments/horse) and subsequently received oral administration of acetaminophen (20 mg/kg). Am J Vet Res . 2013 Aug;74(8):1103-10.

Effect of dopamine solution on isolated strips of longitudinal smooth muscle obtained from the midjejunum of 6 horses that were euthanized for reasons other than gastrointestinal or other systemic disease after the muscle strips were preincubated with domperidone solution (10⁻⁴M; circles) or vehicle solution (rectangles) for 20 minutes. Am J Vet Res . 2013 Aug;74(8):1103-10.