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Irsogladine maleate

Cat. No. M6836
Irsogladine maleate Structure
Synonym:

Dicloguamine maleate; MN1695

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Biological Activity

Irsogladine maleate is a phosphodiesterase 4 (PDE4) inhibitor that displays gastroprotective properties. Prevents gastric mucosal injury induced by monochloramine and ischemia-reperfusion. Activates gap-junctional intercellular communication improving gastric mucosal barrier function. Inhibits superoxide production in human neutrophils and inhibits in vitro and in vivo angiogenesis.

Chemical Information
Molecular Weight 372.18
Formula C9H7Cl2N5.C4H4O4
CAS Number 84504-69-8
Solubility (25°C) DMSO 37.22 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Irikura, et al. J Biol Chem. Biochemical, functional and pharmacological characterization of AT-56, an orally active and selective inhibitor of lipocalin-type prostaglandin D synthase.

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Keywords: Irsogladine maleate, Dicloguamine maleate; MN1695 supplier, inhibitors, activators


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