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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
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
Lesinurad Related Products
| Related Targets | OAT1 OAT3 URAT1 | Click to Expand |
|---|---|---|
| Related Compound Libraries | FDA-approved Drug Library Natural Product Library Ion Channel Ligand Library Exosome Secretion Related Compound Library Calcium Channel Blocker Library | Click to Expand |
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 |
|
| 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 Information & 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 |
DMSO : 80 mg/mL ( (197.88 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.) Ethanol : 54 mg/mL Water : Insoluble |
Molecular Weight Calculator |
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In vivo Add solvents to the product individually and in order. |
In vivo Formulation Calculator |
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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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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.
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