1. Membrane Transporter/Ion Channel
  2. URAT1
  3. Lesinurad

Lesinurad (Synonyms: RDEA594)

Cat. No.: HY-15258 Purity: 99.99%
Handling Instructions

Lesinurad is a URAT1 and OAT inhibitor, is determined to be a substrate for the kidney transporters OAT1 and OAT3 with Km values of 0.85 and 2 µM, respectively.

For research use only. We do not sell to patients.

Lesinurad Chemical Structure

Lesinurad Chemical Structure

CAS No. : 878672-00-5

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10 mM * 1 mL in DMSO USD 66 In-stock
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10 mg USD 84 In-stock
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50 mg USD 228 In-stock
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100 mg USD 312 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

Lesinurad is a URAT1 and OAT inhibitor, is determined to be a substrate for the kidney transporters OAT1 and OAT3 with Km values of 0.85 and 2 µM, respectively.

IC50 & Target

Km: 0.85 µM (OAT1), 2 µM (OAT3)[1]

In Vitro

Lesinurad is a novel selective uric acid reabsorption inhibitor (SURI). Lesinurad is determined to be a substrate for the kidney transporters organic anion transporter (OAT1) and OAT3 with Km values of 0.85 and 2 µM, respectively[1]. Lesinurad (RDEA594) is a URAT1 and OAT inhibitor, which increases proximal renal tubule urate excretion[2]. Lesinurad (RDEA594) is a potential uric acid lowering agent througn inhibition of uric acid reuptake, and exhibits favorable p450 profiles, inhibits CYP2C9 and CYP2C8 with IC50 of 14.4 μM and 16.2 μM, respectively. IC50s of Lesinurad are all above 100 µM for CYP1A2, CYP2C19,and CYP2D6[3].

In Vivo

Lesinurad (RDEA594) shows better pharmacokinetics than its pro-drug RDEA806. The 100 mg dose of Lesinurad exhibits a phamacological effect in the range of that produced by 300 mg to 800 mg single doses of RDEA806[3].

Clinical Trial
Molecular Weight

404.28

Formula

C₁₇H₁₄BrN₃O₂S

CAS No.

878672-00-5

SMILES

BrC1=NN=C(SCC(O)=O)N1C2=C3C(C=CC=C3)=C(C4CC4)C=C2

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (247.35 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4735 mL 12.3677 mL 24.7353 mL
5 mM 0.4947 mL 2.4735 mL 4.9471 mL
10 mM 0.2474 mL 1.2368 mL 2.4735 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.18 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.18 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.18 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[1]

Validated oocytes, HEK293, MDCK-II, Caco-2 or MDCK-MDR1 cell systems are used to study the interaction of Lesinurad with membrane transporters localized to the kidney (OAT1, OAT3, OCT2, MATE1, and MATE2K) or liver (P-gp, BCRP, OATP1B1, OATP1B3, and OCT1). Xenopus laevis oocytes are injected with OAT1 or OAT3 cRNA or control (water) while HEK293 cells are stably transfected with MATE1, MATE2K, or vector and MDCK-II cells with hOATP1B1, hOATP1B3, hOCT1, hOCT2, or vector. The MDCKII cell line is stably transfected with the human MDR1 gene to create a P-gp cell line. The interaction of Lesinurad with BCRP relied on the endogenous expression in Caco-2 cells. All cells are cultured with growth medium according to standard methodology. In order to determine whether Lesinurad is a substrate for a transporter, cells are incubated with [14C]-labeled Lesinurad at various concentrations and the amount of Lesinurad taken up by the cells determined by subtracting the uptake in vector cells from that in the transfected cells. The uptake of a [3H]-labeled known substrate of the transporter served as the positive control. Inhibition of a transporter by Lesinurad is determined by incubating cells with a fixed concentration of [3H]-labeled known substrate and various concentrations of unlabeled Lesinurad. Inhibition by a known inhibitor of each transporter served as the positive control. Cells are incubated for the appropriate amount of time. All reactions are terminated by the addition of ice-cold medium. The cells are then rinsed with medium and lysed[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: 99.99%

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