Ilaprazole

Cas No.:	172152-36-2
Chemical Name:	1H-Benzimidazole,2-[[(4-methoxy-3-methyl-2-pyridinyl)methyl]sulfinyl]-6-(1H-pyrrol-1-yl)-
Synonyms:	2-[(4-methoxy-3-methyl-pyridin-2-yl)methylsulfinyl]-5-pyrrol-1-yl-3H-benzoimidazole;1H-Benzimidazole,2-[[(4-methoxy-3-methyl-2-pyridinyl)methyl]sulfinyl]-6-(1H-pyrrol-1-yl)-;2-[(4-methoxy-3-methylpyridin-2-yl)methylsulfinyl]-6-pyrrol-1-yl-1H-benzimidazole;2-[[(4-methoxy-3-methyl-2-pyridinyl)methyl]sulfinyl]-6-(1H-pyrrol-1-yl)-1H-Benzimidazole;2-{[(4-methoxy-3-methylpyridin-2-yl)methyl]sulfinyl}-5-(1H-pyrrol-1-yl)-1H-benzimidazole;4-(4,4,5,5-TETRAMETHYL-1,3,2-DIOXABOROLAN-2-YL)-1H-PYRAZOLE-1-ACETAMIDE;Ilaprazole;2-[[(4-methoxy-3-methyl)-2-pyridinyl]methylsulfinyl]-5-(1H-pyrol-1-yl)-1H-benzimidazole;2-{[(4-methoxy-3-methylpyridin-2-yl)methyl]sulfinyl}-6-(1h-pyrrol-1-yl)-1h-benzimidazole;Aldenon;Ilaprazole [INN];IY81149;IY-81149;Ilaprazole(IY 81149)
SMILES:	O=S(C1=NC2=CC=C(N3C=CC=C3)C=C2N1)CC4=NC=CC(OC)=C4C
Formula:	C19H18N4O2S
M.Wt:	366.43682
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

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