| CAS NO: | 2465-59-0 |
| 包装 | 价格(元) |
| 500mg | 电议 |
| 1g | 电议 |
| 5g | 电议 |
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 152.1 |
| Cas No. | 2465-59-0 |
| Formula | C5H4N4O2 |
| Synonyms | Alloxanthine|NSC 76239 |
| Solubility | insoluble in EtOH; insoluble in H2O; ≥5.16 mg/mL in DMSO with ultrasonic |
| Chemical Name | 1H-pyrazolo[3,4-d]pyrimidine-4,6(5H,7H)-dione |
| Canonical SMILES | O=C1C2=C(NN=C2)NC(N1)=O |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
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.
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