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Cipamfylline

Cat. No. M8308
Cipamfylline Structure
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Biological Activity

Cipamfylline is a PDE4 inhibitor that has been shown to cause a cellular redistribution of PDE4A4 into accretion foci, through an association with the ubiquitin scaffolding protein p62.

Chemical Information
Molecular Weight 275.31
Formula C13H17N5O2
CAS Number 132210-43-6
Solubility (25°C) DMSO: ≥10 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] Helen Nankervis, et al. Scoping systematic review of treatments for eczema

[2] Wolfgang Bumer, et al. Highly selective phosphodiesterase 4 inhibitors for the treatment of allergic skin diseases and psoriasis

[3] M Bays, et al. Gateways to clinical trials

[4] M Kucharekova, et al. The effect of the PDE-4 inhibitor (cipamfylline) in two human models of irritant contact dermatitis

[5] C E M Griffiths, et al. Randomized comparison of the type 4 phosphodiesterase inhibitor cipamfylline cream, cream vehicle and hydrocortisone 17-butyrate cream for the treatment of atopic dermatitis

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