| Identification | Back Directory | [Name]
Ilaprazole sodium | [CAS]
172152-50-0 | [Synonyms]
IY-81149 sodium
Ilaprazole sodium
Sodium ilaprazole
Ilaprazole sodium USP/EP/BP | [Molecular Formula]
C19H19N4NaO2S | [MDL Number]
MFCD30719460 | [MOL File]
172152-50-0.mol | [Molecular Weight]
390.44 |
| Chemical Properties | Back Directory | [storage temp. ]
4°C, protect from light | [form ]
Solid | [color ]
White to off-white | [InChI]
InChI=1S/C19H18N4O2S.Na.H/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,(H,21,22);; | [InChIKey]
VZAVMHHKFOFGOE-UHFFFAOYSA-N | [SMILES]
S(C1=NC2=CC=C(N3C=CC=C3)C=C2N1)(=O)CC1N=CC=C(OC)C=1C.[NaH] | [CAS DataBase Reference]
172152-50-0 |
| Hazard Information | Back Directory | [Uses]
After oral administration, Ilaprazole sodium selectively enters the gastric parietal cells and is converted into an active metabolite of sulfenamide, which interacts with the sulfhydryl group on the H+/K+-ATPase to form a covalent combination of disulfide bonds, irreversibly inhibiting H+/K+- ATPase, which inhibits gastric acid secretion. | [in vitro]
On cumulation of 14C-aminopyrine in histamine stimulated parietal cells, the IC 50 of Ilaprazole (IY-81149) sodium is 9 nM. | [in vivo]
Ilaprazole sodium (3-30 mg/kg; i.d.) dose-dependently inhibits gastric acid secretion[1].
In anesthetized rats, Ilaprazole sodium dose-dependently increases gastric pH which is lowered by histamine infusion. In the case of i.v. injection, the ED50 of Ilaprazole sodium and Omeprazole is 1.2 and 1.4 mg/kg and in the case of i.d. administration, the ED50 of Ilaprazole sodium and omeprazole is 3.9 and 4.1 mg/kg, respectively. Ilaprazole sodium also significantly inhibits pentagastrin-stimulated gastric secretion. Its ED50 is 2.1 mg/kg and that of Omeprazole was 3.5 mg/kg with i.d. administration. In the case of i.v. injection, Ilaprazole sodium is equipotent to Omeprazole. Ilaprazole sodium also inhibits gastric acid secretion strongly in fistular rats. The ED50 of Ilaprazole sodium administered intraduodenally is 0.43 mg/kg and that of omeprazole Is 0.68 mg/kg[1]. | Animal Model: | Male SD rat (after pylorus ligation)[1] | | Dosage: | 3, 10, 30 mg/kg | | Administration: | Intraduodenally | | Result: | The acid output and volume significantly inhibited by about 60 % and 46 % at 3 mg/kg were s, respectively. At 30 mg/kg, it showed 93 % and 73 % inhibition on acid output and volume, respectively.
|
| [target]
| Target | Value | Proton pump
() | | H(+) /K(+)-ATPase
(in rabbit parietal cell preparation) | 6 μM |
| [storage]
4°C, protect from light |
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