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Motapizone

Cat. No. M42567
Motapizone Structure
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Biological Activity

Motapizone (NAT 05-239) is a selective PDE3 inhibitor.

Chemical Information
Molecular Weight 260.31
Formula C12H12N4OS
CAS Number 90697-57-7
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] Ralph Theo Schermuly et al. Respir Res. Lung vasodilatory response to inhaled iloprost in experimental pulmonary hypertension: amplification by different type phosphodiesterase inhibitors

[2] Christian Martin et al. Naunyn Schmiedebergs Arch Pharmacol. Airway relaxant and anti-inflammatory properties of a PDE4 inhibitor with low affinity for the high-affinity rolipram binding site

[3] F Gantner et al. J Pharmacol Exp Ther. Protection from T cell-mediated murine liver failure by phosphodiesterase inhibitors

[4] K F Rabe et al. Am J Physiol. Identification of PDE isozymes in human pulmonary artery and effect of selective PDE inhibitors

[5] V Schulz et al. Eur J Clin Pharmacol. Inhibition of thrombocyte aggregation by oral motapizone and other drugs

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