1、Product Data SheetIlaprazoleCat. No.: HY-101664CAS No.: 172152-36-2分式: CHNOS分量: 366.44作靶點: Proton Pump作通路: Membrane Transporter/Ion Channel儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 35 mg/mL (95.51 mM)Ethanol : 12.5 mg/mL (34.11 mM; Need ultrasonic)* means

2、 soluble, but saturation unknown.SolventMass1 mg 5 mg 10 mgConcentration制備儲備液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備液；旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 儲存時，請在 6 個內(nèi)使，-20C

3、儲存時，請在 1 個內(nèi)使。體內(nèi)實驗請根據(jù)您的實驗動物和給藥式選擇適當(dāng)?shù)娜芙獍?。以下溶解案都請先按?In Vitro 式配制澄清的儲備液，再依次添加助溶劑：為保證實驗結(jié)果的可靠性，澄 的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使； 以下溶劑前顯的百分 指該溶劑在您配制終溶液中的體積占；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的式助溶1. 請依序添加每種溶劑： 10% EtOH 40% PEG300 5% Tween-80 45% salineSolubility: 1.25 mg/mL (3.41 mM); Clear solution此案可獲得 1

4、.25 mg/mL (3.41 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 12.5 mg/mL 的澄 EtOH 儲備液加到 400 L PEG300 中，混合均勻；向上述體系中加50 L Tween-80，混合均勻；然后繼續(xù)加 450 L 理鹽定容 1 mL。2. 請依序添加每種溶劑： 10% EtOH 90% (20% SBE-CD in saline)Solubility: 1.25 mg/mL (3.41 mM); Clear solutionPage 1 of 2 www.MedChemE此案可獲得 1.25 mg/mL (3.41 mM，飽和度未知) 的

5、澄清溶液。以 1 mL 作液為例，取 100 L 12.5 mg/mL 的澄 EtOH 儲備液加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合均勻。3. 請依序添加每種溶劑： 10% EtOH 90% corn oilSolubility: 1.25 mg/mL (3.41 mM); Clear solution此案可獲得 1.25 mg/mL (3.41 mM，飽和度未知) 的澄 溶液，此案不適于實驗周 期在半個以上的實驗。以 1 mL 作液為例，取 100 L 12.5 mg/mL 的澄 EtOH 儲備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTIVITY物

6、活性 Ilaprazole (IY-81149)質(zhì)泵抑制劑；抑制H+/K+-ATPase的IC50值為6.0 M。IC & 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 IC50 of pumpinhibitory activity of 6.0 M. The IC50 of ilaprazole is 9.0 nM on cumulation of 14

7、C-aminopyrine in histaminestimulated parietal cells1.體內(nèi)研究 In pylorus-ligated rats, ilaprazole shows strong inhibitory activity against gastric acid secretion. The ED50 of ilaprazoleadministered intraduodenally is 1.6 mg/kg. For oral administration, the ED50 of ilaprazole is 1.94 mg/kg. Ilaprazole al

8、so 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. administration1. Intravenous ilaprazole exhibitshigh antiulcer activity in a dose-dependent manner. Ilaprazole a

9、t a dose of 3 mg/kg decreases ulcer number andindex to the same extent as 20 mg/kg esomeprazole. Moreover, the potency of intravenous ilaprazole is superior tothat of intragastric ilaprazole. In anesthetized rats, the inhibitory effect of intravenous ilaprazole on histamine-inducedacid secretion is

10、faster and longer-lasting than that of intraduodenal ilaprazole2.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. Ilaprazole is dissolved in

11、DMSO. Allincubations contain less than 1 % DMSO. The enzyme reaction is started by the addition of 0.5 mL of a mixturecontaining 4 mM MgCl2, 4 mM ATP, and 80 mM imidazole buffer (pH 7.4), with or without 20 mM KCl. Afterincubation for 15 min at 37 C the reaction is terminated by adding 1 mL of 24 %

12、trichloroacetic acid, and theinorganic phosphorus from the ATP is measured1.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 ligation, the animals areAd

13、ministration 1 sacrificed, and the gastric juice is collected and analyzed for acid output. Pentagastrin 60 g/kg is given intravenouslyto rats 30 min before the pylorus is ligated1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Kwon D, et

14、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.Page 2 of 3 www.MedChemE2. 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.McePdfHeigh