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Allopurinol

Cat. No. M3302
Allopurinol Structure
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500mg USD 50  USD50 In stock
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Quality Control & Documentation
Biological Activity

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.

Chemical Information
Molecular Weight 136.11
Formula C5H4N4O
CAS Number 315-30-0
Form Solid
Solubility (25°C) DMSO 20 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] Richard O Day, et al. Allopurinol: insights from studies of dose-response relationships

[2] Lisa K Stamp, et al. Allopurinol and kidney function: An update

[3] Anita Kelkar, et al. Allopurinol as a cardiovascular drug

[4] Arie Markel. Allopurinol-induced DRESS syndrome

[5] M McNaughton Collins, et al. Allopurinol for chronic prostatitis

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Keywords: Allopurinol supplier, Xanthine Oxidase, inhibitors, activators


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