1. Membrane Transporter/Ion Channel Cell Cycle/DNA Damage
  2. Proton Pump TOPK
  3. Ilaprazole

Ilaprazole  (Synonyms: IY-81149)

Cat. No.: HY-101664 Purity: 99.97%
COA Handling Instructions

Ilaprazole (IY-81149) is an orally active proton pump inhibitor. Ilaprazole irreversibly inhibits H+/K+-ATPase in a dose-dependent manner with an IC50 of pump inhibitory activity of 6 μM in rabbit parietal cell preparation. Ilaprazole is used for the research of gastric ulcers. Ilaprazole is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor.

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

Ilaprazole Chemical Structure

Ilaprazole Chemical Structure

CAS No. : 172152-36-2

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Customer Review

Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Ilaprazole (IY-81149) is an orally active proton pump inhibitor. Ilaprazole irreversibly inhibits H+/K+-ATPase in a dose-dependent manner with an IC50 of pump inhibitory activity of 6 μM in rabbit parietal cell preparation. Ilaprazole is used for the research of gastric ulcers. Ilaprazole is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor[1][2].

IC50 & Target

IC50: 6.0 μM (H+/K+-ATPase)[1]

In Vitro

On cumulation of 14C-aminopyrine in histamine stimulated parietal cells, the IC50 of Ilaprazole (IY-81149) sodium is 9 nM[1].

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

In Vivo

Ilaprazole (3-30 mg/kg; i.d.) dose-dependently inhibits gastric acid secretion[1].
In anesthetized rats, Ilaprazole dose-dependently increased gastric pH which was lowered by histamine infusion. In the case of i.v. injection, the ED50 of Ilaprazole and omeprazole is 1.2 and 1.4 mg/kg and in the case of i.d. administration, the ED50 of Ilaprazole and omeprazole is 3.9 and 4.1 mg/kg, respectively. Ilaprazole also significantly inhibits pentagastrin-stimulated gastric secretion. Its ED50 is 2.1 mg/kg and that of Omeprazole is 3.5 mg/kg with i.d. administration. In the case of i.v. injection, Ilaprazole is equipotent to Omeprazole. Ilaprazole also inhibits gastric acid secretion strongly in fistular rats. The ED50 of Ilaprazole administered intraduodenally is 0.43 mg/kg and that of Omeprazole is 0.68 mg/kg[1].

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

Animal Model: Male SD rat (after pylorus ligation)[1]
Dosage: 3, 10, 30 mg/kg
Administration: Intraduodenally
Result: The acid output and volume significantly inhibited by about 60 % and 46 % at 3 mg/kg were s, respectively. At 30 mg/kg, it showed 93 % and 73 % inhibition on acid output and volume, respectively.
Clinical Trial
Molecular Weight

366.44

Formula

C19H18N4O2S

CAS No.
Appearance

Solid

Color

Off-white to gray

SMILES

O=S(C1=NC2=CC=C(N3C=CC=C3)C=C2N1)CC4=NC=CC(OC)=C4C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years

*The compound is unstable in solutions, freshly prepared is recommended.

Solvent & Solubility
In Vitro: 

DMSO : ≥ 35 mg/mL (95.51 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : 5 mg/mL (13.64 mM; Need ultrasonic)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7290 mL 13.6448 mL 27.2896 mL
5 mM 0.5458 mL 2.7290 mL 5.4579 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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% EtOH    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 1.25 mg/mL (3.41 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (12.5 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% EtOH    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 1.25 mg/mL (3.41 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (12.5 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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 compound is unstable in solutions, freshly prepared is recommended.

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: 99.97%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
Ethanol / DMSO 1 mM 2.7290 mL 13.6448 mL 27.2896 mL 68.2240 mL
5 mM 0.5458 mL 2.7290 mL 5.4579 mL 13.6448 mL
10 mM 0.2729 mL 1.3645 mL 2.7290 mL 6.8224 mL
DMSO 15 mM 0.1819 mL 0.9097 mL 1.8193 mL 4.5483 mL
20 mM 0.1364 mL 0.6822 mL 1.3645 mL 3.4112 mL
25 mM 0.1092 mL 0.5458 mL 1.0916 mL 2.7290 mL
30 mM 0.0910 mL 0.4548 mL 0.9097 mL 2.2741 mL
40 mM 0.0682 mL 0.3411 mL 0.6822 mL 1.7056 mL
50 mM 0.0546 mL 0.2729 mL 0.5458 mL 1.3645 mL
60 mM 0.0455 mL 0.2274 mL 0.4548 mL 1.1371 mL
80 mM 0.0341 mL 0.1706 mL 0.3411 mL 0.8528 mL
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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.

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