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Allopurinol

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Chemical Structure| 315-30-0 同义名 : 别嘌呤醇
CAS号 : 315-30-0
货号 : A124580
分子式 : C5H4N4O
纯度 : 98%
分子量 : 136.112
MDL号 : -
存储条件:

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 12 mg/mL(88.16 mM),配合低频超声,并水浴加热至45℃助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 1 mg/mL(7.35 mM),配合低频超声,并调节pH至11

动物实验配方:
生物活性
描述 Allopurinol is a purine analog; it is a structural isomer of hypoxanthine (a naturally occurring purine in the body) and is an inhibitor of the enzyme xanthine oxidase with an IC50 of 7.82±0.12 μM. Allopurinol is almost completely metabolized to oxypurinol within two hours of oral administration [3]. Allopurinol is the most commonly used urate lowering therapy in the management of gout[4]. Allopurinol is generally well tolerated. The initial dosage of allopurinol should be low, particularly in patients with renal impairment. The dose should then be increased slowly until plasma concentrations of urate are sufficient to dissolve monosodium urate crystals (≤0.36 mmol/L)[5]. Along with preventing uric acid formation, allopurinol also has the ability to behave as a free radical scavenger of the superoxide anions and free radicals released during uric acid formation. Allopurinol has also been shown to decrease oxidative stress and ameliorate the morbidity and mortality of congestive heart failure patients by possibly improving mechano-energetic uncoupling, with the enhancement of myocardial contractility and the left ventricular ejection fraction[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

7.35mL

1.47mL

0.73mL

36.73mL

7.35mL

3.67mL

73.47mL

14.69mL

7.35mL

参考文献

[1]Kang SM, Lim S, et al. Allopurinol modulates reactive oxygen species generation and Ca2+ overload in ischemia-reperfused heart and hypoxia-reoxygenated cardiomyocytes. Eur J Pharmacol. 2006 Mar 27;535(1-3):212-9.

[2]Horiuchi H, Ota M, et al. Allopurinol induces renal toxicity by impairing pyrimidine metabolism in mice. Life Sci. 2000 Apr 14;66(21):2051-70.

[3]Pacher P, Nivorozhkin A, Szabó C. Therapeutic effects of xanthine oxidase inhibitors: renaissance half a century after the discovery of allopurinol. Pharmacol Rev. 2006 Mar;58(1):87-114

[4]Stamp LK, Chapman PT, Palmer SC. Allopurinol and kidney function: An update. Joint Bone Spine. 2016 Jan;83(1):19-24

[5]Day RO, Kannangara DR, Stocker SL, Carland JE, Williams KM, Graham GG. Allopurinol: insights from studies of dose-response relationships. Expert Opin Drug Metab Toxicol. 2017 Apr;13(4):449-462

[6]Kelkar A, Kuo A, Frishman WH. Allopurinol as a cardiovascular drug. Cardiol Rev. 2011 Nov-Dec;19(6):265-71