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Proxyphylline

Cat. No. M5057
Proxyphylline Structure
Size Price Availability Quantity
100mg USD 65  USD65 In stock
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Quality Control & Documentation
Biological Activity

Proxyphylline is a methylxanthine and derivative of theophylline. Proxyphylline relaxes smooth muscles, particularly bronchial muscles. This xanthine most likely exerts its effect by inhibiting cAMP or cGMP phosphodiesterases, thereby increasing levels of the second messenger cAMP or cGMP intracellularly. Other mode of actions include an adenosine antagonistic effect on the activity of CD4 lymphocytes and mediator release from mast cells thereby decreasing lung sensitivity to allergens and other substances that cause inflammation. Proxyphylline also acts as a CNS stimulant and exerts a positive chronotropic and inotropic effect on the heart.

Chemical Information
Molecular Weight 238.24
Formula C10H14N4O3
CAS Number 603-00-9
Form Solid
Solubility (25°C) DMSO
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] Małgorzata Gizińska, et al. Antifungal polybrominated proxyphylline derivative induces Candida albicans calcineurin stress response in Galleria mellonella

[2] Paweł Borowiecki, et al. Synthesis of novel proxyphylline derivatives with dual Anti-Candida albicans and anticancer activity

[3] Paweł Borowiecki, et al. Chemoenzymatic Synthesis of Proxyphylline Enantiomers

[4] Dimitrios N Soulas, et al. Proxyphylline release kinetics from symmetrical three-layer silicone rubber matrices: effect of different excipients in the outer rate-controlling layers

[5] K Selvig, et al. Metabolism of proxyphylline in man. Isolation and identification of metabolites in urine

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  Catalog
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