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Allopurinol ROS inhibitor

Cat.No.S1630

Allopurinol is a purine analog inhibitor of the enzyme xanthine oxidase, used to treat gout or kidney stones, and to decrease levels of uric acid.
Allopurinol  ROS inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 136.11

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Quality Control

Batch: Purity: 99.98%
99.98

Solubility

In vitro
Batch:

DMSO : 27 mg/mL (198.36 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 3 mg/mL

Water : Insoluble

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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 136.11 Formula

C5H4N4O

Storage (From the date of receipt)
CAS No. 315-30-0 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles C1=NNC2=C1C(=O)NC=N2

Mechanism of Action

Targets/IC50/Ki
xanthine oxidase
In vitro
Allopurinol reverses the increased xanthine oxidase activity in ischemia-reperfusion injury of neonatal rat hearts. This compound (10 mM) treatment suppresses xanthine oxidase activity induced by hypoxia-reoxygenation injury and the production of reactive oxygen species. It also decreases the concentration of intracellular Ca2+ increased by enhanced xanthine oxidase activity.
In vivo
Allopurinol shows abnormal pyrimidine metabolism together with renal toxicity which could be ameliorated by uridine, indicating that this compound essentially causes pyrimidine metabolism abnormality leading to renal impairment in normal mice. It increases urinary OD excretion to an extent similar to that in normal mice administered the same dose of this chemical in DNFB-sensitized mice. This compound 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. It prevents early alcohol-induced liver injury in rats, most likely by preventing oxidant-dependent activation of NF-kappaB. This chemical 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. It almost completely inhibits hepatic xanthine oxidase and dehydrogenase activity, but only high doses prevents the increase of the mitochondrial GSSG content.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/10734182/
  • [5] https://pubmed.ncbi.nlm.nih.gov/2262912/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05665699 Recruiting
Gout
InventisBio Co. Ltd
April 17 2023 Phase 2
NCT05193838 Unknown status
Dilated Cardiomyopathy
Assiut University
May 1 2022 --
NCT05360628 Completed
Healthy
InventisBio Co. Ltd
November 1 2021 Early Phase 1
NCT04853615 Not yet recruiting
SGLT2i Kideny Protection Against Contrast in Diabetic Kidney
Fayoum University|Cairo University
July 1 2021 --

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