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Furafylline

Cat. No. M5059
Furafylline Structure
Size Price Availability Quantity
1mg USD 179  USD179 In stock
5mg USD 539  USD539 In stock
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Quality Control
Biological Activity

Furafylline was a potent, non-competitive inhibitor of high affinity phenacetin O-deethylase activity of microsomal fractions of human liver, a reaction catalysed by P450IA2, with an IC50 value of 0.07 microM. Furafylline had either very little or no effect on human monooxygenase activities catalysed by other isoenzymes of P450, including P450IID1, P450IIC, P450IIA.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 260.25
Formula C12H12N4O3
CAS Number 80288-49-9
Purity 99.78%
Solubility DMSO >10 mg/mL
Storage at -20°C
References

[1] Yang J,et.al. Comp Biochem Physiol C Toxicol Pharmacol. Characterization of chicken cytochrome P450 1A4 and 1A5: inter-paralog comparisons of substrate preference and inhibitor selectivity.

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Keywords: Furafylline supplier, Cytochrome P450 (e.g. CYP17), inhibitors

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