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Cat. No. Name Size Price Add Cart
KI0824Irsogladine maleate50 mg$154
Irsogladine maleate250 mg$368

Chemical Characteristic

Product NameIrsogladine maleate
SynonymsGaslon
CAS No.84504-69-8
Molecular Weight 372.16
FormulaC13H11Cl2N5O4
Chemical Structure

Biological activities

Irsogladine maleate is an anti-ulcer drug. Irsogladine maleate displays gastroprotective properties. Irsogladine maleate is an irsogladine salt of maleate. Irsogladine inhibits 7-ethoxyresorufin O-deethylation (CYP1A2) and tolbutamide hydroxylation (CYP2C9) with Ki of 276 and 156 µM, respectively.[1] Irsogladine also increases cAMP formation in a concentration-dependent manner in neutrophils. Irsogladine inhibits concentration-dependently the superoxide (O2-) production induced by various stimuli including formyl-methionyl-leucyl-phenylalanine, opsonized zymosan, guanosine 5閳?[gamma-thio] triphosphate, A23187 and phorbol 12-myristate 13-acetate. Irsogladine prevents the superoxide production in human neutrophils by the increase of cAMP content by PDE 4 inhibition.[2] Irsogladine protects gastric mucosa against various ulcerogenic stimuli through increasing cyclic AMP in surface mucous cells. Irsogladine dose-dependently facilitates gap-junctional intercellular communication (GJIC) in gastric epithelial cells. [3] Irsogladine administered orally significantly prevents in vivo angiogenesis in mice.[4] Irsogladine protects the small intestine against indomethacin-induced lesions.[5]

Protocols

In vivo: Irsogladine is suspended in a 0.5% hydroxy propyl cellulose solution.[5]

References

[1] Nakamura A, et al. Effects of irsogladine on P450-isoform specific activities in human hepatic microsomes. Arzneimittelforschung. 2006, 56(7): 547-552. 閵嗏偓閵嗏偓
[2] Kyoi T, et al. Irsogladine, an anti-ulcer drug, suppresses superoxide production by inhibiting phosphodiesterase type 4 in human neutrophils. Life Sci. 2004, 76(1): 71-83. 閵嗏偓閵嗏偓
[3] Ueda F, et al. Irsogladine activates gap-junctional intercellular communication through M1 muscarinic acetylcholine receptor. J Pharmacol Exp Ther. 1995, 274(2): 815-819. 閵嗏偓閵嗏偓
[4] Sato Y, et al. Irsogladine is a potent inhibitor of angiogenesis. FEBS Lett. 1993, 322(2): 155-158. 閵嗏偓閵嗏偓
[5] Kamei K, et al. Prophylactic effect of irsogladine maleate against indomethacin-induced small intestinal lesions in rats. Dig Dis Sci. 2008, 53(10): 2657-2666. 閵嗏偓閵嗏偓

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