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Ilaprazole sodium

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Ilaprazole sodium Basic information
Product Name:Ilaprazole sodium
Synonyms:Ilaprazole sodium;IY-81149 sodium;Ilaprazole sodium USP/EP/BP;Sodium ilaprazole;oral,Ilaprazole,acid,ulcers,IY 81149,inhibit,IY-81149,TOPK,gastric,Inhibitor,cancer,Ilaprazole sodium,IY81149,pump,Proton Pump;Ilaprazole Sodium Salt;Ilaprazole sodium, 10 mM in DMSO;Ilaprazole Base/Sodium
CAS:172152-50-0
MF:C19H19N4NaO2S
MW:390.44
EINECS:
Product Categories:Inhibitors
Mol File:172152-50-0.mol
Ilaprazole sodium Structure
Ilaprazole sodium Chemical Properties
storage temp. 4°C, protect from light
form Solid
color White to off-white
InChIInChI=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);;
InChIKeyVZAVMHHKFOFGOE-UHFFFAOYSA-N
SMILESS(C1=NC2=CC=C(N3C=CC=C3)C=C2N1)(=O)CC1N=CC=C(OC)C=1C.[NaH]
CAS DataBase Reference172152-50-0
Safety Information
MSDS Information
Ilaprazole sodium Usage And Synthesis
UsesAfter 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
TargetValue
Proton pump
()
H(+) /K(+)-ATPase
(in rabbit parietal cell preparation)
6 μM
Ilaprazole sodium Preparation Products And Raw materials
Tag:Ilaprazole sodium(172152-50-0) Related Product Information
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