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FR221647

Cat. No. M42280
FR221647 Structure
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Biological Activity

FR221647 is an orally active non-nucleoside inhibitor of adenosine deaminase.

Chemical Information
Molecular Weight 259.3
Formula C14H17N3O2
CAS Number 256461-28-6
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] Xiaopian Tian et al. PLoS One. Probing inhibition mechanisms of adenosine deaminase by using molecular dynamics simulations

[2] Tadashi Terasaka et al. Bioorg Med Chem Lett. Structure-based de novo design of non-nucleoside adenosine deaminase inhibitors

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Keywords: FR221647 supplier, Adenosine Deaminase, inhibitors, activators


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