Lesinurad sodium

Catalog No.S5189 Batch:S518901

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Technical Data

Formula

C17H13BrN3NaO2S
Molecular Weight 426.26 CAS No. 1151516-14-1
Solubility (25°C)* In vitro DMSO 85 mg/mL (199.4 mM)
Ethanol 85 mg/mL (199.4 mM)
Water 8 mg/mL (18.76 mM)
In vivo (Add solvents to the product individually and in order)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.

 4.25mg/ml (9.97mM) Taking the 1 mL working solution as an example, add 50 μL of 85 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
Clear solution
5% DMSO 95% Corn oil

Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.

 0.61mg/ml (1.43mM) Taking the 1 mL working solution as an example, add 50 μL of 12.2 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Lesinurad (RDEA-594) sodium 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

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).

Protocol (from reference)

Animal Study:

[2]
  • Animal Models

    Eight-week-old female athymic nude mice of orthotopic pancreatic tumor xenograft model

  • Dosages

    25 mg/kg

  • Administration

    i.p.

References

  • https://pubmed.ncbi.nlm.nih.gov/26951201/
  • https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9036131/

Selleck's Lesinurad sodium Has Been Cited by 1 Publication

Uricosuric Agents Affect Plasma and Kidney Concentration of Adefovir via Inhibition of Oat1 and Mrp2 in Rats [ Biological and Pharmaceutical Bulletin, February 01, 2023, 170-176] PubMed: 36724945

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.