1. Membrane Transporter/Ion Channel
  2. Proton Pump
  3. Ilaprazole

Ilaprazole (Synonyms: IY-81149)

Cat. No.: HY-101664 Purity: >98.0%
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Ilaprazole (IY-81149) is a proton pump inhibitor; inhibits H+/K+-ATPase with an IC50 of 6.0 μM.

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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Description

Ilaprazole (IY-81149) is a proton pump inhibitor; inhibits H+/K+-ATPase with an IC50 of 6.0 μM.

IC50 & Target

IC50: 6.0 μM (H+/K+-ATPase)[1]

In Vitro

In rabbit parietal cells, ilaprazole irreversibly inhibits H+/K+-ATPase in dose-dependent manner with an IC50 of pump inhibitory activity of 6.0 μM. The IC50 of ilaprazole is 9.0 nM on cumulation of 14C-aminopyrine in histamine stimulated parietal cells[1].

In Vivo

In pylorus-ligated rats, ilaprazole shows strong inhibitory activity against gastric acid secretion. The ED50 of ilaprazole administered intraduodenally is 1.6 mg/kg. For oral administration, the ED50 of ilaprazole is 1.94 mg/kg. Ilaprazole also significantly inhibits pentagastrin-stimulated gastric secretion. Its ED50 is 2.1 mg/kg. In Heidenhain pouch dogs, the acid output is completely blocked at 0.3 mg/kg, 135 min after i.v. administration[1]. Intravenous ilaprazole exhibits high antiulcer activity in a dose-dependent manner. Ilaprazole at a dose of 3 mg/kg decreases ulcer number and index to the same extent as 20 mg/kg esomeprazole. Moreover, the potency of intravenous ilaprazole is superior to that of intragastric ilaprazole. In anesthetized rats, the inhibitory effect of intravenous ilaprazole on histamine-induced acid secretion is faster and longer-lasting than that of intraduodenal ilaprazole[2].

Clinical Trial
Molecular Weight

366.44

Formula

C₁₉H₁₈N₄O₂S

CAS No.

172152-36-2

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
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 35 mg/mL (95.51 mM)

*"≥" 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
*Please refer to the solubility information to select the appropriate solvent.
References
Kinase Assay
[1]

About 60 μg enzyme is pre-incubated in a medium consisting of 5 mM imidazole buffer and ilaprazole and omeprazole at concentrations of 0.01, 0.1, 0.5, 1, 5 μM in a final volume of 0.5 mL. Ilaprazole is dissolved in DMSO. All incubations contain less than 1 % DMSO. The enzyme reaction is started by the addition of 0.5 mL of a mixture containing 4 mM MgCl2, 4 mM ATP, and 80 mM imidazole buffer (pH 7.4), with or without 20 mM KCl. After incubation for 15 min at 37 °C the reaction is terminated by adding 1 mL of 24 % trichloroacetic acid, and the inorganic phosphorus from the ATP is measured[1].

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

Animal Administration
[1]

Rats: Rats are treated with 3 mg/kg ilaprazole for 0, 1, 2, 3, 4, 5 and 7 h. 1 h after pylorus ligation, the animals are sacrificed, and the gastric juice is collected and analyzed for acid output. Pentagastrin 60 μg/kg is given intravenously to rats 30 min before the pylorus is ligated[1].

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

References
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Ilaprazole
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