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Allopurinol 315-30-0

Product Description

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Molecular Weight: 136.11 Allopurinol is a xanthine oxidase inhibitor with an IC50 of 7.82±0.12 μM.


Biological Activity


Allopurinol (Zyloprim) is a xanthine oxidase inhibitor with an IC50 of 7.82±0.12 µM.

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±0.13 µM) and its analogues was compared with that by allopurinol (IC50=7.82±0.12 µM). Among these analogues, 2-chloro-6(methylamino)purine (IC50=10.19±0.10 µM) and 4-aminopyrazolo[3,4-d] pyrimidine (IC50=30.26±0.23 µM) were found to be potent Inhibitors of XO.


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


Species Baboon Dog Monkey Rabbit Guinea pig Rat Hamster Mouse
Weight (kg) 12 10 3 1.8 0.4 0.15 0.08 0.02
Body Surface Area (m2) 0.6 0.5 0.24 0.15 0.05 0.025 0.02 0.007
Km factor 20 20 12 12 8 6 5 3

Animal A (mg/kg) = Animal B (mg/kg) multiplied by Animal B Km
Animal A Km



For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) × mouse Km(3) = 11.2 mg/kg
rat Km(6)




Chemical Information







Molecular Weight (MW) 136.11
Formula

C5H4N4O

CAS No. 315-30-0

Storage 3 years -20℃Powder
6 months-80℃in solvent (DMSO, water, etc.)
Synonyms



Solubility (25°C) * In vitro DMSO 27 mg/mL (198.36 mM)
Water 4 mg/mL (29.38 mM)
Ethanol 3 mg/mL (22.04 mM)




Chemical Name 1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one








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