产品说明书

Irsogladine

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Chemical Structure| 57381-26-7 同义名 : Dicloguamine
CAS号 : 57381-26-7
货号 : A130508
分子式 : C9H7Cl2N5
纯度 : 98%
分子量 : 256.091
MDL号 : MFCD00866871
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 115 mg/mL(449.06 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
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

生物活性
靶点

  • AChR

  • PDE
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.90mL

0.78mL

0.39mL

19.52mL

3.90mL

1.95mL

39.05mL

7.81mL

3.90mL
参考文献

[1]Kawasaki Y, Tsuchida A, et al. Irsogladine malate up-regulates gap junctional intercellular communication between pancreatic cancer cells via PKA pathway. Pancreas. 2002 Nov;25(4):373-7.

[2]Ren CJ, Ueda F, et al. Irsogladine maleate inhibits angiogenesis in wild-type and plasminogen activator-deficient mice. J Surg Res. 1998 Jul 1;77(2):126-31.

[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]Onuma W, Tomono S, Miyamoto S, Fujii G, Hamoya T, Fujimoto K, Miyoshi N, Fukai F, Wakabayashi K, Mutoh M. Irsogladine maleate, a gastric mucosal protectant, suppresses intestinal polyp development in Apc-mutant mice. Oncotarget. 2016 Feb 23;7(8):8640-52

[5]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

[6]Zhang X, Tajima K, Kageyama K, Kyoi T. Irsogladine maleate suppresses indomethacin-induced elevation of proinflammatory cytokines and gastric injury in rats. World J Gastroenterol. 2008 Aug 14;14(30):4784-90