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Chemical Structure| 1151516-14-1 Chemical Structure| 1151516-14-1

Structure of Lesinurad sodium
CAS No.: 1151516-14-1

Chemical Structure| 1151516-14-1

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Lesinurad sodium is an inhibitor of URAT1 and OAT and it is also a substrate for the kidney transporters OAT1 and OAT3 with Km values of 0.85 and 2 µM, respectively.

Synonyms: RDEA-594 sodium; Selexipag; Zurampic

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Product Details of Lesinurad sodium

CAS No. :1151516-14-1
Formula : C17H13BrN3NaO2S
M.W : 426.26
SMILES Code : O=C([O-])CSC1=NN=C(Br)N1C2=C3C=CC=CC3=C(C4CC4)C=C2.[Na+]
Synonyms :
RDEA-594 sodium; Selexipag; Zurampic
MDL No. :MFCD24444603
InChI Key :FVYMVLTWIBGEMC-UHFFFAOYSA-M
Pubchem ID :56928182

Safety of Lesinurad sodium

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
HepG2 cells 30 μM 8 hours Evaluate the effect of Lesinurad on PPARγ-regulated gene expression in HepG2 cells, results showed that Lesinurad markedly induced ANGPTL4 expression. Sci Rep. 2018 Sep 10;8(1):13554
3T3-L1 adipocytes 50 μM 14 days Evaluate the effect of Lesinurad on adipocyte differentiation, results showed that Lesinurad did not induce fat accumulation at 50 μM concentration. Sci Rep. 2018 Sep 10;8(1):13554
HEK293T cells 30 μM 12-14 hours Evaluate the activation effect of Lesinurad on PPARγ, results showed that Lesinurad significantly activated PPARγ at 30 μM concentration with an EC50 value of 18.5 ± 0.7 μM. Sci Rep. 2018 Sep 10;8(1):13554
HEK293-derived 293A cells 100 μM 1 minute To evaluate OAT10-mediated urate transport activity and the inhibitory effect of Lesinurad. Results showed Lesinurad significantly inhibited OAT10-mediated urate transport. Front Pharmacol. 2022 Apr 6;13:842717
HEK293-URAT1 cells 0.23 μM Evaluation of the inhibitory effect of Lesinurad sodium and its derivatives on URAT1-mediated uric acid uptake. The IC50 of 1q was 0.23 μM, which is 31-fold more potent than the parent Lesinurad (IC50=7.18 μM). Molecules. 2016 Nov 16;21(11):1543

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Sprague-Dawley rats Gout model Oral 15 mg/kg Once daily for 7 days To assess the pharmacokinetic interaction between LES and ETC when co-administered, results showed an increase in AUC for both drugs Sci Rep. 2025 Apr 2;15(1):11238

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.35mL

0.47mL

0.23mL

11.73mL

2.35mL

1.17mL

23.46mL

4.69mL

2.35mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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