Ilaprazole-IY-81149-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEIlaprazoleCat. No.: HY-101664CAS No.: 172152-36-2Synonyms: IY-81149分式: CHNOS分量: 366.44作靶點(diǎn): Proton Pump作通路: Membrane Transporter/Ion Channel儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 35

2、 mg/mL (95.51 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 2.7290 mL 13.6448 mL 27.2896 mL5 mM 0.5458 mL 2.7290 mL 5.4579 mL10 mM 0.2729 mL 1.3645 mL 2.7290 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Ilaprazole (IY-81149)質(zhì)泵抑制

3、劑；抑制H+/K+-ATPase的IC50值為6.0 M。IC50 & Target IC50: 6.0 M (H+/K+-ATPase) 1體外研究In rabbit parietal cells, ilaprazole irreversibly inhibits H+/K+-ATPase in dose-dependent manner with an IC501/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEof pump inhibitory activity of 6.0 M. The IC50 of ilaprazole is 9.0

4、 nM on cumulation of 14C-aminopyrine inhistamine stimulated parietal cells 1.體內(nèi)研究 In pylorus-ligated rats, ilaprazole shows strong inhibitory activity against gastric acid secretion. The ED50 ofilaprazole administered intraduodenally is 1.6 mg/kg. For oral administration, the ED50 of ilaprazole is 1

5、.94mg/kg. Ilaprazole also significantly inhibits pentagastrin-stimulated gastric secretion. Its ED50 is 2.1 mg/kg. InHeidenhain pouch dogs, the acid output is completely blocked at 0.3 mg/kg, 135 min after i.v. administration1. Intravenous ilaprazole exhibits high antiulcer activity in a dose-depend

6、ent manner. Ilaprazole at a dose of3 mg/kg decreases ulcer number and index to the same extent as 20 mg/kg esomeprazole. Moreover, thepotency of intravenous ilaprazole is superior to that of intragastric ilaprazole. In anesthetized rats, theinhibitory effect of intravenous ilaprazole on histamine-in

7、duced acid secretion is faster and longer-lasting thanthat of intraduodenal ilaprazole 2.PROTOCOLKinase Assay 1 About 60 g enzyme is pre-incubated in a medium consisting of 5 mM imidazole buffer and ilaprazole andomeprazole at concentrations of 0.01, 0.1, 0.5, 1, 5 M in a final volume of 0.5 mL. Ila

8、prazole is dissolved inDMSO. All incubations contain less than 1 % DMSO. The enzyme reaction is started by the addition of 0.5mL of a mixture containing 4 mM MgCl2, 4 mM ATP, and 80 mM imidazole buffer (pH 7.4), with or without 20mM KCl. After incubation for 15 min at 37 C the reaction is terminated

9、 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 Rats: Rats are treated with 3 mg/kg ilaprazole for 0, 1, 2, 3, 4, 5 and 7 h. 1 h after pylorus li

10、gation, theAdministration 1 animals are sacrificed, and the gastric juice is collected and analyzed for acid output. Pentagastrin 60 g/kgis 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 onl

11、y.REFERENCES1. Kwon D, et al. Effects of IY-81149, a newly developed proton pump inhibitor, on gastric acid secretion in vitro and in vivo.Arzneimittelforschung. 2001;51(3):204-13.2. Yu G, et al. Intravenous ilaprazole is more potent than oral ilaprazole against gastric lesions in rats. Dig Dis Sci. 2014 Oct;59(10):2417-22.McePdfHeightCaution: Product has not