172152-36-2
172152-36-2 structure
- Name: Ilaprazole
- Chemical Name: 2-[(4-methoxy-3-methylpyridin-2-yl)methylsulfinyl]-6-pyrrol-1-yl-1H-benzimidazole
- CAS Number: 172152-36-2
- Molecular Formula: C19H18N4O2S
- Molecular Weight: 366.437
- Catalog: API Digestive system medication Inhibition of gastric acid secretion
- Create Date: 2018-03-20 08:00:00
- Modify Date: 2024-01-02 14:41:28
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Ilaprazole (IY-81149) is a proton pump inhibitor; inhibits H+/K+-ATPase with an IC50 of 6.0 μM.
| Name | 2-[(4-methoxy-3-methylpyridin-2-yl)methylsulfinyl]-6-pyrrol-1-yl-1H-benzimidazole |
|---|---|
| Synonyms |
2-{[(4-Methoxy-3-methyl-2-pyridinyl)methyl]sulfinyl}-5-(1H-pyrrol-1-yl)-1H-benzimidazole
Aldenon UNII:776Q6XX45J 2-{[(4-methoxy-3-methylpyridin-2-yl)methyl]sulfinyl}-6-(1h-pyrrol-1-yl)-1h-benzimidazole 2-[[(4-methoxy-3-methyl)-2-pyridinyl]methylsulfinyl]-5-(1H-pyrol-1-yl)-1H-benzimidazole Ilaprazole [INN] 1H-Benzimidazole, 2-[[(4-methoxy-3-methyl-2-pyridinyl)methyl]sulfinyl]-6-(1H-pyrrol-1-yl)- Ilaprazole Noltec |
| Description | Ilaprazole (IY-81149) is a proton pump inhibitor; inhibits H+/K+-ATPase with an IC50 of 6.0 μM. |
|---|---|
| Related Catalog | |
| 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]. |
| Kinase Assay | 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]. |
| Animal Admin | 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]. |
| References |
| Density | 1.4±0.1 g/cm3 |
|---|---|
| Boiling Point | 651.0±65.0 °C at 760 mmHg |
| Molecular Formula | C19H18N4O2S |
| Molecular Weight | 366.437 |
| Flash Point | 347.5±34.3 °C |
| Exact Mass | 366.115051 |
| PSA | 92.01000 |
| LogP | 2.66 |
| Vapour Pressure | 0.0±1.9 mmHg at 25°C |
| Index of Refraction | 1.710 |