Allopurinol (Zyloprim) is a xanthine oxidase inhibitor with an IC50 of 7.82?.12 uM.
Xanthine oxidase is responsible for the successive oxidation of hypoxanthine and xanthine resulting in the production of uric acid, the product of human purine metabolism. The inhibition of XO activity by 6-aminopurine (IC50=10.89?.13 uM) and its analogues was compared with that by allopurinol (IC50=7.82?.12 uM). Among these analogues, 2-chloro-6 (methylamino)purine (IC50=10.19?.10 uM) and 4-aminopyrazolo[3,4-d] pyrimidine (IC50=30.26?.23 uM) were found to be potent inhibitors of XO.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
|Body Surface Area (m2)
|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.
||DMSO 20 mg/mL