1. Neuronal Signaling
    GPCR/G Protein
  2. Cholinesterase (ChE)
    Dopamine Receptor
  3. Itopride hydrochloride

Itopride hydrochloride (Synonyms: HSR803)

Cat. No.: HY-B0732 Purity: 99.85%
Handling Instructions

Itopride (HSR803) hydrochloride is a potent dopamine-2 antagonist and an acetylcholine esterase (AChE) inhibitor. Itopride hydrochloride enhances gastric motility through both antidopaminergic and anti-acetylcholinesterasic actions, can be used as a gastrointestinal prokinetic agent. Itopride can be used for researching gastro-esophageal reflux disease (GERD).

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

Itopride hydrochloride Chemical Structure

Itopride hydrochloride Chemical Structure

CAS No. : 122892-31-3

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10 mM * 1 mL in DMSO USD 55 In-stock
Estimated Time of Arrival: December 31
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ready for reconstitution
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Description

Itopride (HSR803) hydrochloride is a potent dopamine-2 antagonist and an acetylcholine esterase (AChE) inhibitor. Itopride hydrochloride enhances gastric motility through both antidopaminergic and anti-acetylcholinesterasic actions, can be used as a gastrointestinal prokinetic agent. Itopride can be used for researching gastro-esophageal reflux disease (GERD)[1][2].

IC50 & Target

AChE, D2DR[1]

In Vitro

Itopride hydrochloride has prokinetic effects on both the ileum and colon, which are regulated through inhibitory effects on AChE and antagonistic effects on dopamine D2 receptor[3].
Itopride hydrochloride (0.1 nM-1 μM) significantly accelerats the propagation velocity of the peristalsis in ex guinea pig ileum[3].

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

In Vivo

Itopride hydrochloride (30 mg/kg; p.o.) significantly accelerates gastric emptying compared with the vehicle group[4].
Itopride hydrochloride (30 mg/kg; p.o.) displays Cmax of 358 ‰, T1/2 of 24.9 min[4].

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

Animal Model: Male ddY-strain mice (23.7-28.5 g)[2]
Dosage: 3 mg/kg, 10 mg/kg, 30 mg/kg
Administration: Oral administration
Result: Accelerated gastric emptying at 30 mg/kg dose.
Animal Model: Male ddY-strain mice (23.7-28.5 g)[2]
Dosage: 3 mg/kg, 10 mg/kg, 30 mg/kg (Pharmacokinetic Analysis)
Administration: Oral administration
Result: Cmax (358 ‰), T1/2 (24.9 min) at 30 mg/kg dose.
Clinical Trial
Molecular Weight

394.89

Formula

C20H27ClN2O4

CAS No.
SMILES

O=C(NCC1=CC=C(OCCN(C)C)C=C1)C2=CC=C(OC)C(OC)=C2.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (253.24 mM; Need ultrasonic)

H2O : 50 mg/mL (126.62 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5324 mL 12.6618 mL 25.3235 mL
5 mM 0.5065 mL 2.5324 mL 5.0647 mL
10 mM 0.2532 mL 1.2662 mL 2.5324 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 (6.33 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.33 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (6.33 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation
References
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Product Name:
Itopride hydrochloride
Cat. No.:
HY-B0732
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