Oxipurinol
(Synonyms: 羟基嘌呤,Alloxanthine|NSC 76239) 目录号 : GC10827An inhibitor of xanthine oxidase and active metabolite of allopurinol
Cas No.:2465-59-0
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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.
Cas No. | 2465-59-0 | SDF | |
别名 | 羟基嘌呤,Alloxanthine|NSC 76239 | ||
化学名 | 1H-pyrazolo[3,4-d]pyrimidine-4,6(5H,7H)-dione | ||
Canonical SMILES | O=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°C |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 6.5746 mL | 32.8731 mL | 65.7462 mL |
5 mM | 1.3149 mL | 6.5746 mL | 13.1492 mL |
10 mM | 0.6575 mL | 3.2873 mL | 6.5746 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
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1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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