同义名 :	MN1695;Dicloguamine maleate;Irsogladine (maleate)
	CAS号 :	84504-69-8
	货号 :	A299639
	分子式 :	C13H11Cl2N5O4
	纯度 :	98%
	分子量 :	372.163
	MDL号 :	MFCD00873566
	存储条件：	Pure form Inert atmosphere,Room Temperature In solvent -20°C:3-6个月-80°C:12个月
	溶解度 :	-
	动物实验配方：

生物活性

描述

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]. IM increased cell coupling in a dose-dependent manner (0M-10M). Intracellular cAMP level was increased by IM[4]. IM significantly reduced the incidence and maximum severity of oral mucositis in patients treated with 5-FU-chemotherapy[5]. In addition, IM may control A. actinomycetemcomitans-induced gingival inflammation by regulating neutrophil migration and E-cadherin expression in gingival epithelium[6]. The efficacy of irsogladine maleate was found in H. pylori-negative group, suggesting its potential as a protective agent against NSAIDs (nonsteroidal anti-inflammatory drugs) or aspirin-induced peptic ulcer and gastritis[7].

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 ... 展开 >> Kukje Pharm Seongnam-si, Korea, Republic of 收起 <<
NCT02581696	Peptic Ulcer	Phase 1	Completed	-	Korea, Republic of ... 展开 >> The Catholic University of Korea, Seoul St.Mary's Hospital Seoul, Korea, Republic of 收起 <<
NCT02759224	Gastric Ulcer	Phase 1	Completed	-	Korea, Republic of ... 展开 >> The Catholic University of Korea, Seoul St.Mary's Hospital Seoul, Korea, Republic of 收起 <<

实验方案
	1mg	5mg	10mg
1 mM 5 mM 10 mM	2.69mL 0.54mL 0.27mL	13.43mL 2.69mL 1.34mL	26.87mL 5.37mL 2.69mL

参考文献

[1]Nozaki S, Maeda M, et al. Inhibition of breast cancer regrowth and pulmonary metastasis in nude mice by anti-gastric ulcer agent, irsogladine. Breast Cancer Res Treat. 2004 Feb;83(3):195-9. [2]Kyoi T, Kitazawa S, et al. Phosphodiesterase type IV inhibitors prevent ischemia-reperfusion-induced gastric injury in rats. J Pharmacol Sci. 2004 Jul;95(3):321-8. [3]Ren CJ, Ueda F, Roses DF, Harris MN, Mignatti P, Rifkin DB, Shapiro RL. Irsogladine maleate inhibits angiogenesis in wild-type and plasminogen activator-deficient mice. J Surg Res. 1998 Jul 1;77(2):126-31 [4]Kawasaki Y, Tsuchida A, Sasaki T, Yamasaki S, Kuwada Y, Murakami M, Chayama K. Irsogladine malate up-regulates gap junctional intercellular communication between pancreatic cancer cells via PKA pathway. Pancreas. 2002 Nov;25(4):373-7 [5]Nomura M, Kamata M, Kojima H, Hayashi K, Sawada S. Irsogladine maleate reduces the incidence of fluorouracil-based chemotherapy-induced oral mucositis. Ann Oncol. 2013 Apr;24(4):1062-6 [6]Fujita T, Kishimoto A, Shiba H, Hayashida K, Kajiya M, Uchida Y, Matsuda S, Takeda K, Ouhara K, Kawaguchi H, Abiko Y, Kurihara H. Irsogladine maleate regulates neutrophil migration and E-cadherin expression in gingival epithelium stimulated by Aggregatibacter actinomycetemcomitans. Biochem Pharmacol. 2010 May 15;79(10):1496-505 [7]Shim KN, Kim JI, Kim N, Kim SG, Jo YJ, Hong SJ, Shin JE, Kim GH, Park KS, Choi SC, Kwon JG, Kim JH, Kim HJ, Kim JW. The efficacy and safety of irsogladine maleate in nonsteroidal anti-inflammatory drug or aspirin-induced peptic ulcer and gastritis. Korean J Intern Med. 2019 Sep;34(5):1008-1021