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Lesinurad sodium OAT inhibitor

Cat.No.S5189

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 OAT inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 426.26

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

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

Chemical Information, Storage & Stability

Molecular Weight 426.26 Formula

C17H13BrN3NaO2S

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 1151516-14-1 -- Storage of Stock Solutions

Synonyms Selexipag, Zurampic, RDEA-594 sodium Smiles [Na+].[O-]C(=O)CSC1=NN=C(Br)[N]1C2=CC=C(C3CC3)C4=CC=CC=C24

Solubility

In vitro
Batch:

DMSO : 85 mg/mL (199.4 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 85 mg/mL

Water : 8 mg/mL

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Mechanism of Action

Targets/IC50/Ki
URAT1 [1]
OAT1 [1]
(Cell-free assay)
0.85 μM(Km)
OAT3 [1]
(Cell-free assay)
2 μM(Km)
OAT3 [1]
(Cell-free assay)
3.5 μM
OAT1 [1]
(Cell-free assay)
4.3 μM
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]
References

Clinical Trial Information

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

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

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