Irsogladine

Irsogladine is a PDE4 inhibitor and muscarinic acetylcholine receptor binder. Target: PDE4; mACHR 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. Irsogladine inhibits bFGF-induced angiogenesis in wild-type, tPA-knockout, and uPA-knockout mice [1]. Irsogladine up-regulates GJIC between PC cells via regulation of the PKA pathway. It also suggests a useful adjuvant of Irsogladine to pancreatic cancer therapy [2]. irsogladine produces the increase of intracellular cAMP content via non-selective inhibition of PDE isozymes, which may be a key mechanism involved in its gastroprotective actions [3].

Product Specifications

CAS Number

[57381-26-7]

Product Name Alternative

Dicloguamine

UNSPSC

12352005

Hazard Statement

H302, H312, H332

Target

MAChR; Phosphodiesterase (PDE)

Type

Reference compound

Related Pathways

GPCR/G Protein; Metabolic Enzyme/Protease; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/Irsogladine.html

Concentration

10mM

Purity

99.88

Solubility

DMSO : 120 mg/mL (ultrasonic) |H2O : < 0.1 mg/mL (ultrasonic)

Smiles

NC1=NC(N)=NC(C2=CC(Cl)=CC=C2Cl)=N1

Molecular Formula

C9H7Cl2N5

Molecular Weight

256.09

Precautions

H302, H312, H332

References & Citations

[1]Ren, C.J., et al., Irsogladine maleate inhibits angiogenesis in wild-type and plasminogen activator-deficient mice. J Surg Res, 1998. 77 (2) : p. 126-31.|[2]Kawasaki, Y., et al., Irsogladine malate up-regulates gap junctional intercellular communication between pancreatic cancer cells via PKA pathway. Pancreas, 2002. 25 (4) : p. 373-7.|[3]Kyoi, T., et al., Phosphodiesterase inhibition by a gastroprotective agent irsogladine: preferential blockade of cAMP hydrolysis. Life Sci, 2004. 75 (15) : p. 1833-42.