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。
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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。 |
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]. |
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 << |
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 |
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 |