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马来酸伊索拉定 /Irsogladine maleate {[allProObj[0].p_purity_real_show]}

货号:A299639 同义名: MN1695;Dicloguamine maleate

Irsogladine maleate是一种 PDE4 抑制剂,并可与毒蕈碱乙酰胆碱受体结合,常用于消化系统相关疾病的研究。

Irsogladine maleate 化学结构 CAS号:84504-69-8
Irsogladine maleate 化学结构
CAS号:84504-69-8
Irsogladine maleate 3D分子结构
CAS号:84504-69-8
Irsogladine maleate 化学结构 CAS号:84504-69-8
Irsogladine maleate 3D分子结构 CAS号:84504-69-8
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Irsogladine maleate 纯度/质量文件 产品仅供科研

货号:A299639 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 PDE PDE1 PDE10A PDE2 PDE3 PDE4 PDE5 PDE6 其他靶点 纯度
Doxofylline 99+%
Deltarasin +++

PDEδ , Kd: 38 nM

99+%
7-(2,3-Dihydroxypropyl)theophylline 98%
Aminophylline +

PDE, IC50: 0.12 mM

98+%
Anagrelide HCl 99%+
Irsogladine mAChR,AChR 99%
PF-8380 +++

Autotaxin, IC50: 2.8 nM

99%+
Dipyridamole 98%
Balipodect ++++

PDE10A, IC50: 0.3 nM

99%+
PF-2545920 ++++

PDE10A, IC50: 0.37 nM

97%
Luteolin +

PDE1, Ki: 15.0 μM

++

PDE2, Ki: 6.4 μM

+

PDE3, Ki: 13.9 μM

+

PDE4, Ki: 11.1 μM

+

PDE5, Ki: 9.5 μM

98%
Milrinone ++

PDE2, IC50: 5.2 μM

++

PDE3, IC50: 2.1 μM

ATPase 99%
Pimobendan ++

PDE3, IC50: 0.32 μM

98%
Cilostazol ++

PDE3, IC50: 0.2 μM

98%
Fenspiride HCl +

PDE3, pIC50: 3.44

+

PDE4, pIC50: 4.16

99% (HPLC)
(S)-(+)-Rolipram ++

PDE4, IC50: 0.75 μM

99% (HPLC)
Apremilast +++

PDE4, IC50: 74 nM

98%
GSK256066 ++++

PDE4B, IC50: 3.2 pM

98+%
Roflumilast ++++

PDE4A1, IC50: 0.7 nM

PDE4A4, IC50: 4.3 nM

99%
Rolipram +++

PDE4B, IC50: 130 nM

99%+
Cilomilast +++

HPDE4, IC50: 120 nM

LPDE4, IC50: 100 nM

99%
Avanafil ++++

PDE5, IC50: 1 nM

98%
Vardenafil HCl Trihydrate ++++

PDE5, IC50: 0.7 nM

98%
Tadalafil ++++

PDE5, IC50: 1.8 nM

98%
Icariin ++

PDE5, IC50: 0.432 μM

98%
Sildenafil +++

PDE6, IC50: 33 nM

98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Irsogladine maleate 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].

Irsogladine maleate 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 <<

Irsogladine maleate 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

Irsogladine maleate 实验方案

计算器
存储液制备 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

Irsogladine maleate 技术信息

CAS号84504-69-8
分子式C13H11Cl2N5O4
分子量 372.163
别名 MN1695;Dicloguamine maleate;Irsogladine (maleate)
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Inert atmosphere,Room Temperature

溶解度
动物实验配方
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