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: 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

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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 Active not recruiting 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 lnformation & 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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