Irsogladine maleate (Dicloguamine maleate)
(Synonyms: 马来酸伊索拉定; Dicloguamine maleate; MN1695) 目录号 : GC33878
A gastroprotective agent
Cas No.:84504-69-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Irsogladine is a gastroprotective agent.1,2,3 It increases transfer of Lucifer yellow CH between isolated rabbit gastric epithelial cells, indicating enhanced gap junction intercellular communication (GJIC).2 Irsogladine (3 mg/kg) inhibits gastric mucosal lesion formation and decreases in gastric mucosal blood flow induced by monochloramine in rats, effects that can be prevented by the nitric oxide synthase inhibitor L-NAME .1 It also inhibits superoxide anion production induced by fMLP and increases cAMP levels in isolated human neutrophils in a concentration-dependent manner, similar to the phosphodiesterase 4 (PDE4) inhibitor rolipram .3
1.Kyoi, T., Oka, M., Noda, K., et al.Irsogladine prevents monochloramine-induced gastric mucosal lesions by improving the decrease in mucosal blood flow due to the disturbance of nitric oxide synthesis in ratsJ. Pharmacol. Sci.93(3)314-320(2003) 2.Ueda, F., Ban, K., and Ishima, T.Irsogladine activates gap-junctional intercellular communication through M1 muscarinic acetylcholine receptorJ. Pharm. Exp. Ther.274(2)815-819(1995) 3.Kyoi, T., Noda, K., Oka, M., et al.Irsogladine, an anti-ulcer drug, suppresses superoxide production by inhibiting phosphodiesterase type 4 in human neutrophilsLife Sci.76(1)71-83(2004)
| Cas No. | 84504-69-8 | SDF | |
| 别名 | 马来酸伊索拉定; Dicloguamine maleate; MN1695 | ||
| Canonical SMILES | O=C(O)/C=C\C(O)=O.NC1=NC(N)=NC(C2=CC(Cl)=CC=C2Cl)=N1 | ||
| 分子式 | C13H11Cl2N5O4 | 分子量 | 372.16 |
| 溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2) (1:3): 0.25 mg/ml | 储存条件 | Store at -20°C |
| 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 | 2.687 mL | 13.4351 mL | 26.8702 mL |
| 5 mM | 0.5374 mL | 2.687 mL | 5.374 mL |
| 10 mM | 0.2687 mL | 1.3435 mL | 2.687 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。
[Protective effect of Dicloguamine maleate (MN-1695) on HCl-induced gastric mucosal damage in rats--histologic studies]
Nihon Yakurigaku Zasshi 1987 May;89(5):279-84.PMID:3623330DOI:10.1254/fpj.89.279
Effect of MN-1695, a new cytoprotective antiulcer agent, on 0.2 N HCl-induced gastric surface epithelial cell damage was investigated by optical and transmission electron microscopy in rats. Tissue examination after five minutes exposure to 0.2 N HCl showed extensive damage of the surface epithelial cells: dilatation of intercellular spaces including marked edema of lamina propria. It was found that MN-1695 (3 mg/kg) pretreatment prevented such 0.2 N HCl-induced damage of the surface epithelial cells, and it reduced the percentage of damaged mucosa, but not significantly.