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| 100mg |
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Purity: ≥98%
Lesinurad sodium (formerly known as RDEA594; RDEA-594; trade name Zurampic), the sodium salt of lesinurad, is a selective inhibitor of URAT1 (urate transporter 1) and OAT (organic anion transporter) approved in 2015 for treating high blood uric acid levels associated with gout. It is also called SURI (selective uric acid reabsorption inhibitor). Lesinurad reduces the reuptake of uric acid from urine to blood circulation, thus lowering urate (uric acid) levels in the plasma.
| ln Vitro |
Lesinurad is a new type of SURI, or selective uric acid reabsorption inhibitor. With Km values of 0.85 and 2 µM, respectively, lesinurad was found to be a substrate for the renal transporters organic anion transporter (OAT1) and OAT3 [1]. The OAT and URAT1 inhibitor lesinurad (RDEA594) raises urate excretion from proximal tubular tubules [2]. Lesinurad (RDEA594) is a potentially effective urate-lowering drug that suppresses uric acid reuptake to inhibit CYP2C9 and CYP2C8, and has strong p450 properties, with IC50 values of 14.4 μM and 16.2 μM, respectively. For CYP1A2, CYP2C19, and CYP2D6, lesinurad has an IC50 greater than 100 µM [3].
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| ln Vivo |
Compared to its prodrug, RDEA806, lesinurad (RDEA594) exhibits superior pharmacokinetics. Lesinurad at 100 mg has pharmacological effects comparable to those of a single dose of RDEA806 at 300–800 mg [3].
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| References |
[1]. Shen Z, et al. In Vitro and In Vivo Interaction Studies Between Lesinurad, a Selective Urate Reabsorption Inhibitor, and Major Liver or Kidney Transporters. Clin Drug Investig. 2016 Jun;36(6):443-52
[2]. Sattui SE, et al. Treatment of hyperuricemia in gout: current therapeutic options, latest developments and clinical implications. Ther Adv Musculoskelet Dis. 2016 Aug;8(4):145-59. [3]. L.Yeh, et al. RDEA594, a potential uric acid lowering agent througn inhibition of uric acid reuptake ,shows better pharmacokinetics rhan its prodrug RDEA806. 2008 ACR/ARHP Annual Scientific Meeting, 24-29 October 2008, USA |
| Molecular Formula |
C17H14BRN3O2S
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| Molecular Weight |
426.26
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| CAS # |
1151516-14-1
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| Related CAS # |
Lesinurad;878672-00-5
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| SMILES |
O=C(O[Na])CSC1=NN=C(Br)N1C2=C3C=CC=CC3=C(C4CC4)C=C2
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (5.86 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (5.86 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: 2.5 mg/mL (5.86 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3460 mL | 11.7299 mL | 23.4599 mL | |
| 5 mM | 0.4692 mL | 2.3460 mL | 4.6920 mL | |
| 10 mM | 0.2346 mL | 1.1730 mL | 2.3460 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Median plasma concentration profiles for total atorvastatin (including metabolites) following a single oral dose of atorvastatin 40mg in the absence or presence of a single dose of lesinurad 200mg (a) or 400mg (b), and plasma concentration profile of metformin following a single dose of metformin 850mg (c) or plasma concentration profile of furosemide following a single dose of furosemide 40mg (d) in the absence or presence of a single dose of lesinurad 400mg.Clin Drug Investig.2016 Jun;36(6):443-52. |
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 Uric acid pathway and action site of urate-lowering therapies. *Drugs in italics are agents still under development or still not approved. **Dashed arrow representing lack of metabolic step in humans, due to evolutionary loss of uricase enzyme. |
 enal anion transporters involved in urate reabsorption in the proximal tubule and action sites of existing and novel uricosuric agents. *Drugs in italics are agents still under development or still not approved. |
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