| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
| Targets |
Ilaprazole sodium targets the gastric H+/K+-ATPase (proton pump) in parietal cells, irreversibly inhibiting acid secretion. It also inhibits T cell origin protein kinase (TOPK). The compound is activated in acidic parietal cell compartments to form a sulfenamide that covalently inhibits H+/K+ ATPase.
|
|---|---|
| ln Vitro |
In histamine-stimulated parietal cells, ilaprazole (IY-81149) sodium has an IC50 of 9 nM for 14C-aminopyrine accumulation [1].
In histamine-stimulated parietal cells, ilaprazole sodium has an IC50 of 9 nM for 14C-aminopyrine accumulation. In rabbit parietal cell preparations, it irreversibly inhibits H+/K+-ATPase with an IC50 of 6 μM. |
| ln Vivo |
Gastric acid secretion is dose-dependently inhibited by linaprozole sodium (3–30 mg/kg; id) [1]. Histamine infusion lowered stomach pH in sedated rats, but ilaprazole sodium dose-dependently raised it in intravenous injection cases. The injected doses of omeprazole (1.4 mg/kg) and sodium omeprazole (1.2 mg/kg) are the corresponding ED50s. The ED50s of omeprazole (4.1 mg/kg) and linaprazole sodium (3.9 mg/kg) when given, respectively. Significant inhibition of pentagastrin-stimulated gastric secretion is also observed with ilaprazole sodium. Omeprazole's ED50 is 3.5 mg/kg, whereas its is 2.1 mg/kg. when administering an intravenous injection. In fistula rats, ilaprazole sodium also significantly reduces the release of stomach acid. The ED50 for omeprazole is 0.68 mg/kg and for linaprazole sodium is 0.43 mg/kg when administered intraduodenally[1].
In male SD rats (after pylorus ligation), ilaprazole sodium (3, 10, 30 mg/kg; intraduodenal) dose-dependently inhibits gastric acid secretion. At 3 mg/kg, acid output and volume are inhibited by about 60% and 46%, respectively; at 30 mg/kg, inhibition reaches 93% and 73%. In fistula rats, the intraduodenal ED50 is 0.43 mg/kg. |
| Enzyme Assay |
In vitro enzyme assays typically measure H+/K+-ATPase inhibition in rabbit parietal cell preparations. The enzyme activity is assessed by measuring proton transport or ATP hydrolysis in the presence of varying concentrations of ilaprazole sodium to determine IC50 values.
|
| Cell Assay |
Cell-based assays use histamine-stimulated parietal cells to measure 14C-aminopyrine accumulation as an indicator of acid secretion inhibition. IC50 values are determined by treating cells with increasing concentrations of ilaprazole sodium and quantifying the reduction in aminopyrine uptake.
|
| Animal Protocol |
Animal/Disease Models: Male SD rat (after pylorus ligation)[1]
Doses: 3, 10, 30 mg/kg Route of Administration: Intraduodenally Experimental Results: The acid output and volume Dramatically inhibited by about 60 % and 46 % at 3 mg/kg were s, respectively. At 30 mg/kg, it demonstrated 93 % and 73 % inhibition on acid output and volume, respectively. In vivo efficacy is evaluated in male SD rats after pylorus ligation. Ilaprazole sodium is administered intraduodenally at doses of 3, 10, and 30 mg/kg. Gastric acid output and volume are measured to assess the inhibitory effect on acid secretion. |
| ADME/Pharmacokinetics |
Ilaprazole sodium is orally bioactive. In sedated rats, intravenous injection of ilaprazole sodium dose-dependently raises stomach pH. The ED50 for intravenous administration is 1.2 mg/kg. The compound is activated in acidic environments and accumulates in parietal cells.
|
| Toxicity/Toxicokinetics |
Preclinical toxicity data for ilaprazole sodium are typical of proton pump inhibitors. Long-term use of PPIs is associated with potential risks including vitamin B12 deficiency, bone fractures, and kidney disease. Ilaprazole sodium should be handled with standard laboratory safety precautions. Detailed toxicological profiles are available in the reference literature.
|
| References |
|
| Additional Infomation |
Ilaprazole sodium is a substituted benzimidazole prodrug and a selective, irreversible proton pump inhibitor. It is utilized in research on gastric ulcer models, acid-related disorders, and the pharmacodynamics of PPI mechanisms. The compound is also a potent TOPK inhibitor, suggesting additional research applications beyond acid suppression.
|
| Molecular Formula |
C19H17N4NAO2S
|
|---|---|
| Molecular Weight |
388.42
|
| Exact Mass |
388.096
|
| CAS # |
172152-50-0
|
| Related CAS # |
Ilaprazole;172152-36-2;Ilaprazole sodium hydrate;2322264-11-7
|
| PubChem CID |
121595900
|
| Appearance |
White to off-white solid powder
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
27
|
| Complexity |
508
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
ZQGDDMFDBZPGCD-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C19H17N4O2S.Na/c1-13-17(20-8-7-18(13)25-2)12-26(24)19-21-15-6-5-14(11-16(15)22-19)23-9-3-4-10-23;/h3-11H,12H2,1-2H3;/q-1;+1
|
| Chemical Name |
sodium;2-[(4-methoxy-3-methylpyridin-2-yl)methylsulfinyl]-5-pyrrol-1-ylbenzimidazol-3-ide
|
| 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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : 41.67 mg/mL (107.28 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.36 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 20.8 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: ≥ 2.08 mg/mL (5.36 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 20.8 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.36 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5745 mL | 12.8727 mL | 25.7453 mL | |
| 5 mM | 0.5149 mL | 2.5745 mL | 5.1491 mL | |
| 10 mM | 0.2575 mL | 1.2873 mL | 2.5745 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.
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.
(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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
