research use only

Ilaprazole Proton Pump inhibitor

Name: Ilaprazole
Brand: Selleck Chemicals
SKU: S3666
Availability: InStock
Rating: 5 (3 reviews)

Cat.No.S3666

Ilaprazole (IY-81149) is a new proton pump inhibitor (PPI) used in the treatment of dyspepsia, peptic ulcer disease (PUD), gastroesophageal reflux disease (GORD/GERD) and duodenal ulcer. It inhibits H+/K+-ATPase with an IC50 of 6.0 μM.

Chemical Structure

Molecular Weight: 366.44

Jump to

Quality Control

Batch: S366601 DMSO]73 mg/mL]false]Ethanol]14 mg/mL]false]Water]Insoluble]false Purity: 99.50%

Cited in Nature Medicine for its top-tier quality
COA
HPLC
SDS
Datasheet

99.50

Related Targets	CFTR CRM1 CD markers AChR Calcium Channel Sodium Channel Potassium Channel GABA Receptor TRP Channel ATPase
Other Proton Pump Inhibitors	Bafilomycin A1 (Baf-A1) Tenatoprazole Ilaprazole sodium Revaprazan Hydrochloride PF-3716556 Ufiprazole

Solubility

In vitro
Batch:

DMSO : 73 mg/mL (199.21 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 14 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an 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 the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	366.44	Formula	C₁₉H₁₈N₄O₂S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	172152-36-2	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	IY-81149			Smiles	CC1=C(C=CN=C1CS(=O)C2=NC3=C(N2)C=C(C=C3)N4C=CC=C4)OC

Mechanism of Action

Targets/IC₅₀/Ki	Proton pump H+/K+-ATPase (Cell-free assay) 6 μM TOPK 111 μM(Kd)
In vitro	Ilaprazole inhibited TOPK activities with high affinity and selectivity. In vitro studies showed that this compound inhibited TOPK activities in HCT116, ES-2, A549, SW1990 cancer cells. It was also found to induce the cleavage of poly-(ADP-ribose) polymerase (PARP), a DNA repair regulatory protein. In rabbit parietal cell preparation, this chemical irreversibly inhibited H+/K+-ATPase in dose-dependent manner with an IC50 of pump inhibitory activity of 6.0×10-6 mol/l.
In vivo	Ilaprazole could suppress tumor growth by inhibiting TOPK activities in vivo. The phosphorylations of histone H3 (Ser10) were significantly inhibited in this compound-treated tumor tissues. The toxicological data showed that the LD50 of this chemical was more than 5000 mg/kg in rats. In pylorus-ligated rats, this compound had a strong and long-lasting antisecretory activity despite of its instability in acidic solution. It strongly inhibited secretagogues stimulated gastric acid secretion in rats and dogs.
References	[1] https://pubmed.ncbi.nlm.nih.gov/28388576/ [2] https://pubmed.ncbi.nlm.nih.gov/11304936/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05617651	Not yet recruiting	Pharmacokinetics	Il-Yang Pharm. Co. Ltd.	November 30 2024	Phase 1
NCT05558150	Completed	Drug Interaction Potentiation	Il-Yang Pharm. Co. Ltd.	November 10 2022	Phase 1
NCT05509543	Recruiting	Pharmacokinetics	Il-Yang Pharm. Co. Ltd.	August 24 2022	Phase 1
NCT03099876	Unknown status	Helicobacter Pylori Infection	Il-Yang Pharm. Co. Ltd.	March 1 2017	--

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):