| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg | |||
| Other Sizes |
| Targets |
Ilaprazole sodium hydrate targets the gastric H+/K+-ATPase (proton pump), irreversibly inhibiting acid secretion. It also inhibits T cell origin protein kinase (TOPK). Additionally, it has potential antiviral activity by blocking the release of infectious herpes simplex virus (HSV)-1/2 from Vero cells in culture.
|
|---|---|
| ln Vitro |
For 14C-aminopyrine accumulation in histamine-stimulated parietal cells, ilaprazole (IY-81149) sodium hydrate exhibits an IC50 of 9 nM [1].
In rabbit parietal cell preparations, ilaprazole sodium hydrate irreversibly inhibits H+/K+-ATPase in a dose-dependent manner with an IC50 of 6.0 × 10⁻⁶ mol/L at pH 7.4. This is the primary in vitro activity measurement for this compound. |
| ln Vivo |
Gastric acid secretion is dose-dependently inhibited by linaprozole sodium hydrate (3–30 mg/kg; id) [1]. When intravenous injection was used, the pH of the stomach was lowered by histamine infusion whereas the pH of the stomach was dose-dependently raised by ilaprazole sodium hydrate in anesthetized rats. The injection-specific ED50s for omeprazole and iprazole sodium hydrate are 1.4 and 1.2 mg/kg, respectively. The ED50s of omeprazole (4.1 mg/kg) and ilaprazole sodium hydrate (3.9 mg/kg) when given, respectively. Additionally, pentagastrin-stimulated gastric secretion is greatly inhibited by iloprostezole sodium hydrate. 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 hydrate also significantly reduces stomach acid output. The ED50 for omeprazole is 0.68 mg/kg and for linaprazole sodium hydrate is 0.43 mg/kg when administered intraduodenally[1].
In male SD rats (after pylorus ligation), ilaprazole sodium hydrate (3, 10, 30 mg/kg; intraduodenal) significantly inhibits gastric acid secretion and volume. This demonstrates its in vivo efficacy as a proton pump inhibitor in animal models of gastric acid hypersecretion. |
| Enzyme Assay |
In vitro enzyme assays measure H+/K+-ATPase inhibition in rabbit parietal cell preparations. The enzyme activity is assessed by quantifying proton transport or ATP hydrolysis in the presence of varying concentrations of ilaprazole sodium hydrate to determine the IC50.
|
| Cell Assay |
Cell-based assays for the antiviral activity use Vero cell cultures infected with HSV-1/2. The compound's ability to block infectious virus release and HSV particle transport is measured. For the PPI activity, histamine-stimulated parietal cells are used to assess acid secretion inhibition.
|
| 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 as a PPI is evaluated in male SD rats after pylorus ligation. Ilaprazole sodium hydrate is administered intraduodenally at doses of 3, 10, and 30 mg/kg. Gastric acid output and volume are measured to quantify the inhibitory effect on acid secretion. |
| ADME/Pharmacokinetics |
Ilaprazole sodium hydrate is orally bioactive. It irreversibly inhibits H+/K+-ATPase in a dose-dependent manner. The compound is a weak base that accumulates in acidic environments. Pharmacokinetic properties are expected to be similar to those of ilaprazole sodium.
|
| Toxicity/Toxicokinetics |
Preclinical toxicity data for ilaprazole sodium hydrate are typical of proton pump inhibitors. Long-term PPI use is associated with risks including vitamin B12 deficiency and bone fractures. The compound should be handled with standard laboratory safety precautions. Detailed toxicological information is available in the reference literature.
|
| References |
|
| Additional Infomation |
See also: Ilaprazole sodium (preferred).
Ilaprazole sodium hydrate is an orally active proton pump inhibitor with additional TOPK inhibitory and potential antiviral activities. It blocks the release of infectious HSV-1/2 from Vero cells and blocks HSV particle transport. This compound is a valuable research tool for studying acid-related disorders, cancer (via TOPK inhibition), and viral infections. |
| Molecular Formula |
C19H17N4NAO2S
|
|---|---|
| Molecular Weight |
388.418653249741
|
| Exact Mass |
388.096
|
| CAS # |
2322264-11-7
|
| Related CAS # |
Ilaprazole sodium;172152-50-0
|
| PubChem CID |
53353154
|
| Appearance |
White to light yellow 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
|
| SMILES |
CC1=C(C=CN=C1CS(=O)C2=NC3=C([N-]2)C=CC(=C3)N4C=CC=C4)OC.[Na+]
|
| 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-1-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, avoid exposure to moisture. |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| 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
