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伊索拉定 /Irsogladine {[allProObj[0].p_purity_real_show]}

货号:A130508 同义名: Dicloguamine

Irsogladine is a PDE4 inhibitor and muscarinic acetylcholine receptor binder.

Irsogladine 化学结构 CAS号:57381-26-7
Irsogladine 化学结构
CAS号:57381-26-7
Irsogladine 3D分子结构
CAS号:57381-26-7
Irsogladine 化学结构 CAS号:57381-26-7
Irsogladine 3D分子结构 CAS号:57381-26-7
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Irsogladine 纯度/质量文件 产品仅供科研

货号:A130508 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 AChR,mAChR 98%
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 98%
Pimobendan ++

PDE3, IC50: 0.32 μM

98%
Cilostazol ++

PDE3, IC50: 0.2 μM

98%
Fenspiride HCl +

PDE3, pIC50: 3.44

+

PDE4, pIC50: 4.16

98%
(S)-(+)-Rolipram ++

PDE4, IC50: 0.75 μM

98%
Apremilast +++

PDE4, IC50: 74 nM

98%
GSK256066 ++++

PDE4B, IC50: 3.2 pM

98+%
Roflumilast ++++

PDE4A4, IC50: 4.3 nM

PDE4A1, IC50: 0.7 nM

99%
Rolipram +++

PDE4B, IC50: 130 nM

99%+
Cilomilast +++

LPDE4, IC50: 100 nM

HPDE4, IC50: 120 nM

98+%
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 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].

Irsogladine 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

Irsogladine 实验方案

计算器
存储液制备 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

Irsogladine 技术信息

CAS号57381-26-7
分子式C9H7Cl2N5
分子量 256.091
别名 Dicloguamine
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,Room temperature

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

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