Home Transmembrane Transporters OAT inhibitor Lesinurad For research use only.

Lesinurad

Synonyms: RDEA 594, RDEA-594, RDEA594

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

Lesinurad Chemical Structure

CAS: 878672-00-5

Selleck's Lesinurad has been cited by 1 publication

Purity & Quality Control

Batch: S464001 DMSO] 80 mg/mL] false] Ethanol] 54 mg/mL] false] Water] Insoluble] false Purity: 99.95%
99.95

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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
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].
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01001338 Completed Gout Ardea Biosciences Inc. October 2009 Phase 2
NCT00955981 Completed Hyperuricemia Ardea Biosciences Inc. July 2009 Phase 2

Chemical lnformation & Solubility

Molecular Weight 404.28 Formula

C17H14BrN3O2S
CAS No. 878672-00-5 SDF Download Lesinurad SDF
Smiles C1CC1C2=CC=C(C3=CC=CC=C23)N4C(=NN=C4Br)SCC(=O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 80 mg/mL ( (197.88 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 54 mg/mL

Water : Insoluble


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In vivo
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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.

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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.

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