Lesinurad

Catalog No.S4640 Synonyms: RDEA 594, RDEA-594, RDEA594

For research use only.

Lesinurad (RDEA-594) is a selective uric acid reabsorption inhibitor (SURI) under investigation for treatment of gout in combination with xanthine oxidase inhibitors. Lesinurad is a URAT1 and OAT inhibitor, is determined to be a substrate for the kidney transporters OAT1 and OAT3 with Km values of 0.85 and 2 µM, respectively.

Lesinurad Chemical Structure

CAS No. 878672-00-5

Selleck's Lesinurad has been cited by 1 Publication

Purity & Quality Control

Choose Selective OAT Inhibitors

Biological Activity

Description Lesinurad (RDEA-594) is a selective uric acid reabsorption inhibitor (SURI) under investigation for treatment of gout in combination with xanthine oxidase inhibitors. Lesinurad is a URAT1 and OAT inhibitor, is determined to be a substrate for the kidney transporters OAT1 and OAT3 with Km values of 0.85 and 2 µM, respectively.
Targets
URAT1 [1]
()
In vitro

Lesinurad inhibits the uric acid transport activity of human URAT1 (hURAT1) at a 20-fold higher potency compared to rat URAT1 (rURAT1), with IC50's of 3.36 and 74.84 μM, respectively. Lesinurad inhibits hURAT1 through an interaction that involves a critical residue, Phe365[1].

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 80 mg/mL
(197.88 mM)
Water Insoluble
Ethanol ''''54 mg/mL

Chemical Information

Molecular Weight 404.28
Formula

C17H14BrN3O2S

CAS No. 878672-00-5
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CC1C2=CC=C(C3=CC=CC=C23)N4C(=NN=C4Br)SCC(=O)O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01001338 Completed Drug: RDEA594|Drug: Placebo|Drug: Allopurinol Gout Ardea Biosciences Inc. October 2009 Phase 2
NCT00955981 Completed Drug: RDEA594|Drug: Placebo Hyperuricemia Ardea Biosciences Inc. July 2009 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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