Ilaprazole (IY-81149)
(Synonyms: 艾普拉唑; IY-81149) 目录号 : GC31347
A gastric proton pump inhibitor
Cas No.:172152-36-2
Sample solution is provided at 25 µL, 10mM.
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Ilaprazole is a proton pump inhibitor that inhibits H+/K+-ATPase activity in isolated rabbit gastric mucosa (IC50 = 6 ?M).1 In vivo, ilaprazole reduces gastric acid secretion induced by pentagastrin or histamine in anesthetized rats (ED50s = 0.38 and 1.2 mg/kg, respectively). It also reduces histamine-induced gastric acid secretion in Heidenhain pouch dogs. Formulations containing ilaprazole have been used in the treatment of peptic ulcers and gastroesophageal reflux disease (GERD).
1.Kwon, D., Chae, J.B., Park, C.W., et al.Effects of IY-81149, a newly developed proton pump inhibitor, on gastric acid secretion in vitro and in vivoArzneimittelforschung51(3)204-213(2001)
Kinase experiment: | 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]. |
Animal experiment: | 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]. |
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. | |
| Cas No. | 172152-36-2 | SDF | |
| 别名 | 艾普拉唑; IY-81149 | ||
| Canonical SMILES | O=S(C1=NC2=CC=C(N3C=CC=C3)C=C2N1)CC4=NC=CC(OC)=C4C | ||
| 分子式 | C19H18N4O2S | 分子量 | 366.44 |
| 溶解度 | DMSO : ≥ 35 mg/mL (95.51 mM) | 储存条件 | Store at -20°C,unstable in solution, ready to use. |
| General tips | 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；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.729 mL | 13.6448 mL | 27.2896 mL |
| 5 mM | 0.5458 mL | 2.729 mL | 5.4579 mL |
| 10 mM | 0.2729 mL | 1.3645 mL | 2.729 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet