|6-(2,5-二氯苯基)-1,3,5-三嗪-2,4-二胺|CsnPharm

CAS No.: 57381-26-7

Irsogladine/伊索拉定 Catalog No. CSN16764

Synonyms: Dicloguamine;伊索拉定

Irsogladine is a PDE4 inhibitor and muscarinic acetylcholine receptor binder.

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技术信息

生物活性

描述Irsogladine (irsogladine maleate) is a PDE4 inhibitor and muscarinic acetylcholine receptor binder. IM (irsogladine maleate) treatment (300 and 500 mg/kg/day) resulted in a dose-dependent reduction of angiogenesis in wild-type mice by 21 and 45.3%, in tPA-deficient mice by 42.6 and 46%, and in uPA-deficient mice by 27.2 and 46% , respectively^[3]. Irsogladine maleate suppresses intestinal polyp formation in Min mice partly through the NF-jB signaling pathway, thus reducing oxidative stress^[4]. IM up-regulates GJIC (gap junctional intercellular communication) between PC (pancreatic cancer) cells via regulation of the PKA pathway^[5]. The mucosal protective effects afforded by irsogladine maleate on gastric injury induced by indomethacin are mediated by inhibition of mucosal proinflammatory cytokine production and neutrophil infiltration, leading to suppression of mucosal inflammation and subsequent tissue destruction^[6].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT03509831	Gastritis	Phase 1	Active, not recruiting	April 2018	Korea, Republic of ... more >> Kukje Pharm Seongnam-si, Korea, Republic of Collapse <<
NCT02759224	Gastric Ulcer	Phase 1	Completed	-	Korea, Republic of ... more >> The Catholic University of Korea, Seoul St.Mary's Hospital Seoul, Korea, Republic of Collapse <<
NCT02581696	Peptic Ulcer	Phase 1	Completed	-	Korea, Republic of ... more >> The Catholic University of Korea, Seoul St.Mary's Hospital Seoul, Korea, Republic of Collapse <<

参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.9049 mL
- 19.5243 mL
- 39.0486 mL
- 5 mM
- 0.7810 mL
- 3.9049 mL
- 7.8097 mL
- 10 mM
- 0.3905 mL
- 1.9524 mL
- 3.9049 mL

技术信息

CAS号

57381-26-7

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C9H7Cl2N5

运输

蓝冰

分子量

256.09

别名

Dicloguamine;伊索拉定

溶解度

DMSO	50.0 mg/mL (195.2 mM) warming
Water	insoluble

动物实验配方

IP	2% DMSO+2% Tween80+30% PEG300+water	1 mg/mL	clear
PO	0.5% CMC-Na	82 mg/mL	suspension

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