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抑制剂描述:

产品名称:Allopurinol

产品别名:见爱必信官网

英文别名:Allopurinol

靶点:Xanthine Oxidase

CAS:315-30-0

纯度:>98%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

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.

溶解性:Ethanol :3 mg/mL (22.04 mM)
DMSO :26 mg/mL (191 mM)
Water :4 mg/mL (29.38 mM)

体外研究:

Allopurinol reverses the increased xanthine oxidase activity in ischemia-reperfusion injury of neonatal rat hearts. Allopurinol (10 mM) treatment suppresses xanthine oxidase activity induced by hypoxia-reoxygenation injury and the production of reactive oxygen species. Allopurinol also decreases the concentration of intracellular Ca2+ increased by enhanced xanthine oxidase activity.

体内研究:Allopurinol shows abnormal pyrimidine metabolism together with renal toxicity which could be ameliorated by uridine, indicating that Allopurinol essentially causes pyrimidine metabolism abnormality leading to renal impairment in normal mice. Allopurinol increases urinary OD excretion to an extent similar to that in normal mice administered the same dose of Allopurinol in DNFB-sensitized mice. Allopurinol promotes a clinical improvement which is accompanied by a reduction in the parasitic load in the blood, skin and lymph nodes but, even after long period of allopurinol administration alone, Leishmania may persist in dog tissues in Leishmania-infected dogs. Allopurinol prevents early alcohol-induced liver injury in rats, most likely by preventing oxidant-dependent activation of NF-kappaB. Allopurinol protects dose-dependently against acetaminophen-induced cell injury, the loss of ATP and the increase of the GSSG content in the total liver and in the mitochondrial compartment without inhibiting reactive metabolite formation in mice. Allopurinol almost completely inhibits hepatic xanthine oxidase and dehydrogenase activity, but only high doses prevents the increase of the mitochondrial GSSG content.

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