84504-69-8
Chemical Structure
Irsogladine maleate
Synonym(s): Dicloguamine maleate; MN1695
- CAS No.: 84504-69-8
- Formula:C13H11Cl2N5O4
- Molecular Weight:372.16
IUPAC Name: 6-(2,5-dichlorophenyl)-1,3,5-triazine-2,4-diamine maleate
InChIKey: PJLVTVAIERNDEQ-BTJKTKAUSA-N
SMILES: O=C(O)/C=C\C(O)=O.NC1=NC(N)=NC(C2=CC(Cl)=CC=C2Cl)=N1
Biological Activity: Irsogladine (Dicloguamine) maleate is an orally active gastric mucosal protective agent and a PDE4 inhibitor. Irsogladine maleate inhibits breast cancer recurrence and lung metastasis in nude mice. Irsogladine maleate inhibits the transcriptional activities of NF-κB and AP-1, suppresses the activities of PDE and PDE4 to elevate intracellular cAMP levels, and activates TRPV1 and KATP channels. Irsogladine maleate enhances iNOS expression, NO production, and the activation of cAMP-responsive elements. Irsogladine maleate inhibits the development and progression of intestinal polyps in Apc-mutant mice. Irsogladine maleate alleviates oxidative stress, increases gastric mucosal blood flow, and stimulates the production of endogenous prostaglandins. Irsogladine maleate promotes insulin secretion in MIN6 cells. Irsogladine maleate inhibits tumor angiogenesis, cancer cell proliferation, and the production of proinflammatory cytokines. Irsogladine maleate exerts protective effects on astrocytes in ethanol/hydrochloric acid-induced gastric ulcers in mice. Irsogladine maleate prevents colitis in IL-10 gene-deficient mice by reducing the production of IL-12 and IL-23. Irsogladine maleate upregulates gap junction intercellular communication in pancreatic cancer cells via the PKA pathway. Irsogladine maleate is applicable to research related to breast cancer, intestinal polyposis, gastric ulcer, spontaneous colitis, glioma, liver cancer, and pancreatic cancer[1][2][3][4][5][6][7][8].
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Irsogladine maleate | 99.75% | Irsogladine (Dicloguamine) maleate is an orally active gastric mucosal protective agent and a PDE4 inhibitor. Irsogladine maleate inhibits breast cancer recurrence and lung metastasis in nude mice. Irsogladine maleate inhibits the transcriptional activities of NF-κB and AP-1, suppresses the activities of PDE and PDE4 to elevate intracellular cAMP levels, and activates TRPV1 and KATP channels. Irsogladine maleate enhances iNOS expression, NO production, and the activation of cAMP-responsive elements. Irsogladine maleate inhibits the development and progression of intestinal polyps in Apc-mutant mice. Irsogladine maleate alleviates oxidative stress, increases gastric mucosal blood flow, and stimulates the production of endogenous prostaglandins. Irsogladine maleate promotes insulin secretion in MIN6 cells. Irsogladine maleate inhibits tumor angiogenesis, cancer cell proliferation, and the production of proinflammatory cytokines. Irsogladine maleate exerts protective effects on astrocytes in ethanol/hydrochloric acid-induced gastric ulcers in mice. Irsogladine maleate prevents colitis in IL-10 gene-deficient mice by reducing the production of IL-12 and IL-23. Irsogladine maleate upregulates gap junction intercellular communication in pancreatic cancer cells via the PKA pathway. Irsogladine maleate is applicable to research related to breast cancer, intestinal polyposis, gastric ulcer, spontaneous colitis, glioma, liver cancer, and pancreatic cancer. | ||||||||||||||||||||
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References
- [1]. Nozaki S, et al. Inhibition of breast cancer regrowth and pulmonary metastasis in nude mice by anti-gastric ulcer agent, irsogladine. Breast Cancer Res Treat. 2004;83(3):195-199. [Content Brief]
- [2]. Onuma W, et al. Irsogladine maleate, a gastric mucosal protectant, suppresses intestinal polyp development in Apc-mutant mice. Oncotarget. 2016;7(8):8640-8652. [Content Brief]
- [3]. Kwon SC, et al. Gastroprotective effects of irsogladine maleate on ethanol/hydrochloric acid induced gastric ulcers in mice. Korean J Intern Med. 2021;36(1):67-75. [Content Brief]
- [4]. Yao J, et al. Irsogladine maleate potentiates the effects of nitric oxide on activation of cAMP signalling pathways and suppression of mesangial cell mitogenesis. Br J Pharmacol. 2007;151(4):457-466. [Content Brief]
- [7]. Ono M, et al. Inhibition of tumor growth and neovascularization by an anti-gastric ulcer agent, irsogladine. Cancer Res. 1996 Apr 1;56(7):1512-6. [Content Brief]
- [8]. Kawasaki Y, et al. Irsogladine malate up-regulates gap junctional intercellular communication between pancreatic cancer cells via PKA pathway. Pancreas. 2002;25(4):373-377. [Content Brief]