Irsogladine - CAS 57381-26-7
Catalog number: 57381-26-7
Category: Inhibitor
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Molecular Formula:
C9H7Cl2N5
Molecular Weight:
256.09
COA:
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Targets:
mAChR
Description:
Irsogladine is a PDE4 inhibitor and muscarinic acetylcholine receptor binder.Irsogladine treatment (300 and 500 mg/kg/day) resulted in a dose-dependent reduction of angiogenesis in wild-type mice by 21 and 45.3% (P < 0.02, P < 0.001), in tPA-deficient mice by 42.6 and 46% (P < 0.001, P < 0.001), and in uPA-deficient mice by 27.2 and 46% (P < 0.05, p < 0.001), respectively.
Purity:
>98%
MSDS:
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InChIKey:
ATCGGEJZONJOCL-UHFFFAOYSA-N
InChI:
InChI=1S/C9H7Cl2N5/c10-4-1-2-6(11)5(3-4)7-14-8(12)16-9(13)15-7/h1-3H,(H4,12,13,14,15,16)
Canonical SMILES:
C1=CC(=C(C=C1Cl)C2=NC(=NC(=N2)N)N)Cl
1.Irsogladine maleate, a gastric mucosal protectant, suppresses intestinal polyp development in Apc-mutant mice.
Onuma W1,2, Tomono S3, Miyamoto S1, Fujii G4, Hamoya T1, Fujimoto K5, Miyoshi N3, Fukai F2, Wakabayashi K3, Mutoh M1,4. Oncotarget. 2016 Feb 23;7(8):8640-52. doi: 10.18632/oncotarget.7082.
This study aimed to identify gastric mucosal protectants that suppress intestinal tumorigenesis in a mouse model. We chose six gastric mucosal protectants (ecabet sodium hydrate, irsogladine maleate, rebamipide, sofalcone, teprenone and troxipide) and examined their effects on the activity of oxidative stress-related transcriptional factors, including AP-1, NF-jB, NRF2, p53 and STAT3, in Caco-2 cells using a luciferase reporter gene assay. Among the six protectants, irsogladine maleate clearly inhibited NF-jB and AP-1 transcriptional activity. Furthermore, the chemopreventive property of irsogladine maleate was examined in a Min mouse model of familial adenomatous polyposis. Treatment with irsogladine maleate at doses of 5 and 50 ppm significantly reduced the number of intestinal polyps to 69% and 66% of the untreated control value, respectively. In these polyps, mRNA levels of the downstream targets of NF-jB, such as IL-1β and IL-6, were decreased by irsogladine maleate treatment.
2.Irsogladine maleate regulates gap junctional intercellular communication-dependent epithelial barrier in human nasal epithelial cells.
Miyata R1, Nomura K, Kakuki T, Takano K, Kohno T, Konno T, Sawada N, Himi T, Kojima T. J Membr Biol. 2015 Apr;248(2):327-36. doi: 10.1007/s00232-015-9774-0. Epub 2015 Feb 5.
The airway epithelium of the human nasal mucosa acts as the first physical barrier that protects against inhaled substances and pathogens. Irsogladine maleate (IM) is an enhancer of gastric mucosal protective factors via upregulation of gap junctional intercellular communication (GJIC). GJIC is thought to participate in the formation of functional tight junctions. However, the effects of IM on GJIC and the epithelial barrier in human nasal epithelial cells (HNECs) remain unknown. To investigate the effects of IM on GJIC and the tight junctional barrier in HNECs, primary cultures of HNECs transfected with human telomerase reverse transcriptase (hTERT-HNECs) were treated with IM and the GJIC inhibitors oleamide and 18β-GA. Some cells were pretreated with IM before treatment with TLR3 ligand poly(I:C) to examine whether IM prevented the changes via TLR3-mediated signal pathways. In hTERT-HNECs, GJIC blockers reduced the expression of tight junction molecules claudin-1, -4, -7, occludin, tricellulin, and JAM-A.
3.Irsogladine improves small-intestinal injuries in regular users of nonsteroidal anti-inflammatory drugs.
Isomura Y1, Yamaji Y1, Yamada A1, Watanabe Y1, Suzuki H1, Kobayashi Y1, Yoshida S1, Watabe H1, Hirata Y1, Yoshida H1, Koike K1. Gastrointest Endosc. 2014 Jul;80(1):118-25. doi: 10.1016/j.gie.2013.12.030. Epub 2014 Feb 8.
BACKGROUND: Nonsteroidal anti-inflammatory drugs (NSAIDs) cause a high frequency of mucosal injuries in the small intestine. However, no reliable intervention, other than cessation of NSAIDs, has been established.
4.Irsogladine Maleate Prevents Colitis in Interleukin-10 Gene-Deficient Mice by Reducing Interleukin-12 and -23 Production.
Nakagawa T1, Katsuno T, Noguchi Y, Mandai Y, Yoshihama S, Saito K, Maruoka D, Matsumura T, Arai M, Yokosuka O. Biol Pharm Bull. 2015;38(11):1681-8. doi: 10.1248/bpb.b15-00189.
Irsogladine maleate (2,4-diamino-6-[2,5-dichlorophenyl]-s-triazine maleate; IM), an anti-peptic ulcer drug, may have a protective effect on the gastrointestinal mucosa. This study investigated the effects of IM on spontaneous colitis in interleukin-10 gene-deficient (IL-10(-/-)) mice. Five-week-old IL-10(-/-) mice were fed a control diet or one containing 100 ppm of IM for 10 weeks. Colonic tissues were evaluated morphologically and histologically. J774A.1 murine monocyte/macrophage cells were incubated with IM after lipopolysaccharide stimulation. mRNA expression was assessed by quantitative polymerase chain reaction (PCR) and protein concentration by enzyme-linked immunosorbent assay (ELISA). Colonic length, weight, and histological scores clearly demonstrated that spontaneous colitis was prevented in IL-10(-/-) mice fed a diet containing IM compared with those fed control diet. Levels of tumor necrosis factor-alpha (TNF-α) (-2.5-fold), IL-1β (-5.
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CAS 57381-26-7 Irsogladine

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