Home Transmembrane Transporters OAT inhibitor Lesinurad sodium For research use only.

Lesinurad sodium

Synonyms: Selexipag, Zurampic, RDEA-594 sodium

Lesinurad (Selexipag, RDEA-594) sodium (Zurampic) is a selective uric acid reabsorption inhibitor (SURI) under investigation for treatment of gout. Lesinurad sodium inhibits the uric acid transporter URAT1 and Kidney transporter OAT with IC50/Km of 4.3 μM/0.85 μM and 3.5 μM/2 μM for OAT1 and OAT3, respectively.

Lesinurad sodium Chemical Structure

Lesinurad sodium Chemical Structure

CAS No. 1151516-14-1

Purity & Quality Control

Batch: S518901 DMSO]85 mg/mL]false]Ethanol]85 mg/mL]false]Water]8 mg/mL]false Purity: 99.96%
99.96

Lesinurad sodium Related Products

Biological Activity

Description Lesinurad (Selexipag, RDEA-594) sodium (Zurampic) is a selective uric acid reabsorption inhibitor (SURI) under investigation for treatment of gout. Lesinurad sodium inhibits the uric acid transporter URAT1 and Kidney transporter OAT with IC50/Km of 4.3 μM/0.85 μM and 3.5 μM/2 μM for OAT1 and OAT3, respectively.
Targets
URAT1 [1] OAT1 [1]
(Cell-free assay)		 OAT3 [1]
(Cell-free assay)		 OAT3 [1]
(Cell-free assay)		 OAT1 [1]
(Cell-free assay)
0.85 μM(Km) 2 μM(Km) 3.5 μM 4.3 μM
In Vivo
In vivo

Lesinurad, a pan-SLC22A inhibitor, reduces epithelial-mesenchymal transition (EMT)-induced metastasis and gemcitabine chemoresistance to prolong survival in mouse models of pancreatic cancer, thus identifying new vulnerabilities for human pancreatic ductal adenocarcinoma (PDAC).[2]
Animal Research Animal Models Eight-week-old female athymic nude mice of orthotopic pancreatic tumor xenograft model
Dosages 25 mg/kg
Administration i.p.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04435782 Terminated
Pulmonary Arterial Hypertension
Actelion
 July 7 2021 Phase 4
NCT04565990 Completed
Hypertension Pulmonary
Actelion
 May 3 2021 Phase 3
NCT04175600 Active not recruiting
Hypertension Pulmonary
Actelion
 January 16 2020 Phase 3
NCT03492177 Active not recruiting
Pulmonary Arterial Hypertension
Actelion
 July 23 2018 Phase 2
NCT03496506 Completed
Healthy Subjects
Actelion
 March 5 2018 Phase 1

Chemical Information & Solubility

Molecular Weight 426.26 Formula

C17H13BrN3NaO2S
CAS No. 1151516-14-1 SDF --
Smiles [Na+].[O-]C(=O)CSC1=NN=C(Br)[N]1C2=CC=C(C3CC3)C4=CC=CC=C24
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 85 mg/mL ( (199.4 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 85 mg/mL

Water : 8 mg/mL


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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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