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BW-A78U

Cat. No. M20590
BW-A78U Structure
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Biological Activity

BW-A78U, an adenine derivative PDE inhibitor, has anticonvulsant activity.

Chemical Information
Molecular Weight 257.27
Formula C13H12FN5
CAS Number 101155-02-6
Solubility (25°C) DMSO 51 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] J J Bourguignon, et al. J Med Chem. 9-Benzyladenines: potent and selective cAMP phosphodiesterase inhibitors

[2] J L Kelley, et al. J Med Chem. Synthesis and anticonvulsant activity of N-benzylpyrrolo[2,3-d]-, -pyrazolo[3,4-d]-, and -triazolo[4,5-d]pyrimidines: imidazole ring-modified analogues of 9-(2-fluorobenzyl)-6-(methylamino)-9H-purine

[3] J L Kelley, et al. J Med Chem. 9-(2-Fluorobenzyl)-6-(methylamino)-9H-purine hydrochloride. Synthesis and anticonvulsant activity

[4] M Willard, et al. Pharmacol Biochem Behav. Anxiolytic and sedative properties of BW A78U, a novel anticonvulsant adenine derivative

[5] G Griebel, et al. Pharmacol Biochem Behav. Behavioral effects of rolipram and structurally related compounds in mice: behavioral sedation of cAMP phosphodiesterase inhibitors

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  Catalog
Abmole Inhibitor Catalog




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