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Lesinurad OAT inhibitor

Cat.No.S4640

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

Chemical Structure

Molecular Weight: 404.28

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Quality Control

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

Chemical Information, Storage & Stability

Molecular Weight 404.28 Formula

C17H14BrN3O2S

 Storage (From the date of receipt)
CAS No. 878672-00-5 Download SDF Storage of Stock Solutions

Synonyms RDEA 594, RDEA-594, RDEA594 Smiles C1CC1C2=CC=C(C3=CC=CC=C23)N4C(=NN=C4Br)SCC(=O)O

Solubility

In vitro
Batch:

DMSO : 80 mg/mL (197.88 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 54 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

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

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Mechanism of Action

Targets/IC50/Ki
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. This compound inhibits hURAT1 through an interaction that involves a critical residue, Phe365[1].
References

Clinical Trial Information

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

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

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