Product Data?SheetIlaprazoleCat. No.:CAS No.:分?式:分?量:作?靶点:作?通路:储存?式:HY-101664172152-36-2C??H??N?O?S366.44Proton PumpMembrane Transporter/Ion ChannelPowderIn solvent-20°C4°C-80°C-20°C3 years2 years6 months1 monthInhibitors?Agonists?Screening Libraries溶解性数据体外实验DMSO : ≥ 35 mg/mL (95.51 mM)Ethanol : 12.5 mg/mL (34.11 mM; Need ultrasonic)* \Mass1 mg5 mg10 mgSolventConcentration制备储备液1 mM5 mM10 mM2.7290 mL0.5458 mL0.2729 mL13.6448 mL2.7290 mL1.3645 mL27.2896 mL5.4579 mL2.7290 mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；?旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存?式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个?内使?，-20°C 储存时，请在 1 个?内使?。体内实验请根据您的实验动物和给药?式选择适当的溶解?案。以下溶解?案都请先按照 In Vitro ?式配制澄清的储备液，再依次添加助溶剂： 为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的?作液，建议您现?现配，当天使?； 以下溶剂前显?的百分?是指该溶剂在您配制终溶液中的体积占?；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的?式助溶1. 请依序添加每种溶剂：?10% EtOH ?? 40% PEG300 ?? 5% Tween-80 ?? 45% salineSolubility: ≥ 1.25 mg/mL (3.41 mM); Clear solution此?案可获得 ≥ 1.25 mg/mL (3.41 mM，饱和度未知) 的澄清溶液。 以 1 mL ?作液为例，取 100 μL 12.5 mg/mL 的澄清 EtOH 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加? 50 μL Tween-80，混合均匀；然后继续加? 450 μL ?理盐?定容? 1 mL。2. 请依序添加每种溶剂：?10% EtOH ?? 90% (20% SBE-β-CD in saline)Solubility: ≥ 1.25 mg/mL (3.41 mM); Clear solutionPage 1 of 2 www.MedChemExpress.cn
此?案可获得 ≥ 1.25 mg/mL (3.41 mM，饱和度未知) 的澄清溶液。 以 1 mL ?作液为例，取 100 μL 12.5 mg/mL 的澄清 EtOH 储备液加到 900 μL 20% 的 SBE-β-CD ?理盐??溶液中，混合均匀。3. 请依序添加每种溶剂：?10% EtOH ?? 90% corn oilSolubility: ≥ 1.25 mg/mL (3.41 mM); Clear solution此?案可获得 ≥ 1.25 mg/mL (3.41 mM，饱和度未知) 的澄清溶液，此?案不适?于实验周期在半个?以上的实验。 以 1 mL ?作液为例，取 100 μL 12.5 mg/mL 的澄清 EtOH 储备液加到 900 μL ??油中，混合均匀。BIOLOGICAL ACTIVITY?物活性IC?? & Target体外研究Ilaprazole (IY-81149)是质?泵抑制剂；抑制H+/K+-ATPase的IC50值为6.0 μM。IC50: 6.0 μM (H+/K+-ATPase)[1]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].体内研究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].PROTOCOLKinase Assay [1]About 60 μg enzyme is pre-incubated in a medium consisting of 5 mM imidazole buffer and ilaprazole and omeprazole at concentrations of 0.01, 0.1, 0.5, 1, 5 μM in a final volume of 0.5 mL. Ilaprazole is dissolved in DMSO. All incubations contain less than 1 % DMSO. The enzyme reaction is started by the addition of 0.5 mL of a mixture containing 4 mM MgCl2, 4 mM ATP, and 80 mM imidazole buffer (pH 7.4), with or without 20 mM KCl. After incubation for 15 min at 37 °C the reaction is terminated 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 Administration [1]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 are sacrificed, and the gastric juice is collected and analyzed for acid output. Pentagastrin 60 μg/kg is 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 only.REFERENCES[1].?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.Page 2 of 3 www.MedChemExpress.cn
[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 been fully validated for medical applications. For research use only.
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