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Oxipurinol
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Oxipurinol图片
CAS NO:2465-59-0
包装与价格:
包装价格(元)
500mg电议
1g电议
5g电议

产品介绍
Oxipurinol (Oxipurinol) 是别嘌醇的主要活性代谢物,是黄嘌呤氧化酶的抑制剂。
Cas No.2465-59-0
别名羟基嘌呤,Alloxanthine|NSC 76239
化学名1H-pyrazolo[3,4-d]pyrimidine-4,6(5H,7H)-dione
Canonical SMILESO=C1C2=C(NN=C2)NC(N1)=O
分子式C5H4N4O2
分子量152.1
溶解度≤3mg/ml in DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Oxipurinol is a xanthine oxidoreductase inhibitor.

Xanthine oxidoreductase (XO), a complex molybdoflavoenzyme present in milk and many other tissues, has been studied for many years. XO is generally recognized as a critical enzyme in purine catabolism.

In vitro: Allopurinol could be rapidly oxidized by XO to its active metabolite oxypurinol (both isosteres of hypoxanthine and xanthine, respectively), which also could inhibit XO. Oxypurinol was identified as a noncompetitive inhibitor of XO; the formation of this compound was reported to be responsible for much of the pharmacological activity of allopurinol. Moreover, both allopurinol and oxypurinol showed free radical scavenging effects in isolated hearts, and exerted cardioprotective effects despite no detectable XO activities [1].

In vivo: Animal study found that in the vasculature of hypercholesterolemic rabbits, oxypurinol treatment led to a decrease in vascular free radical production [1].

Clinical trial: The PK parameters of oxypurinol in subjects with normal renal function were found to be t((1/2)) of 23.3 +/- 6.0 hours, CL/F of 0.31 +/- 0.07 mL/min/kg, V(d)/F of 0.59 +/- 0.16 L/kg, and renal clearance relative to creatinine clearance. Oxypurinol has been found to be cleared almost entirely by urinary excretion and, thus the dosage of allopurinol should be reduced in renal impairment [2].

References:
[1] P.  Pacher, A. Nivorozhkin and C. Szabó. Therapeutic effects of xanthine oxidase inhibitors: Renaissance half a century after the discovery of allopurinol. Pharmacological Reviews 58(1), 87-114 (2006).
[2] Day RO, Graham GG, Hicks M, McLachlan AJ, Stocker SL, Williams KM.  Clinical pharmacokinetics and pharmacodynamics of allopurinol and oxypurinol. Clin Pharmacokinet. 2007;46(8):623-44.