Ilaprazole (Synonyms: IY-81149)

Name: Ilaprazole
Brand: MedChemExpress
SKU: HY-101664
Rating: 4.5 (1 reviews)

Cat. No.: HY-101664 Purity: 99.97%: FAQs
Data Sheet SDS COA Handling Instructions

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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

CAS No. : 172152-36-2

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Based on 1 publication(s) in Google Scholar

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Description

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.

172152-36-2

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
10 mM	0.2729 mL	1.3645 mL	2.7290 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)

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% 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.
Protocol 3

Add each solvent one by one: 10% EtOH 90% Corn Oil
Solubility: ≥ 1.25 mg/mL (3.41 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 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 EtOH stock solution (12.5 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 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%

Select Batch:

Data Sheet (273 KB) SDS (393 KB)

COA (248 KB) HNMR (195 KB) RP-HPLC (445 KB)

Handling Instructions (2659 KB)

References

[1]. Kwon D, et al. Effects of IY-81149, a newly developed proton pump inhibitor, on gastric acid secretion in vitro and in vivo. Arzneimittelforschung. 2001;51(3):204-13. [Content Brief]

[2]. Zheng M, et al. Proton pump inhibitor ilaprazole suppresses cancer growth by targeting T-cell-originated protein kinase. Oncotarget. 2017;8(24):39143-39153. [Content Brief]

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

Ilaprazole Related Classifications

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:

Ilaprazole172152-36-2IY-81149IY81149IY 81149Proton PumpTOPKT-LAK cell-originated protein kinaseoralpumpgastriculcersacidcancerInhibitorinhibitorinhibit

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Ilaprazole (Synonyms: IY-81149)

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Other Forms of Ilaprazole:

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Complete Stock Solution Preparation Table

Ilaprazole Related Classifications

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