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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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1g |
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Purity: ≥98%
Lesinurad (formerly RDEA-594; RDEA594; trade name: Zurampic) is a potent and selective URAT1 (urate transporter 1) inhibitor approved as an anti-gout medication in 2016 by FDA. It can reduce the reuptake of uric acid from urine to blood circulation, thus lowering urate levels in the plasma. It is also an OAT (organic anion transporter) inhibitor thus may cause drug-drug interactions with other medications that are also OAT substrates. Lesinurad belongs to the so called SURI (selective uric acid reabsorption inhibitor).
ln Vitro |
Lesinurad is a brand-new reagent for the selective uric acid reabsorption (SURI). Renal transporters OAT1 and OAT3 were found to utilise lesinurad as a substrate; their Km values were found to be 0.85 and 2 μM, respectively [1]. A URAT1 and OAT dye that raises proximal tubular urate excretion is called lesinurad (RDEA594) [2]. Lesinurad (RDEA594) is a potentially effective urate-lowering drug that inhibits CYP2C9 and CYP2C8 with IC50 values of 14.4 μM and 16.2 μM, respectively, and shows strong p450 characteristics by preventing uric acid re-concentration. Lesinurad has an IC50 of 100 μM against CYP1A2, CYP2C19, and CYP2D6[3].
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ln Vivo |
Compared to its prodrug, RDEA806, lesinurad (RDEA594) exhibits superior pharmacokinetics. The pharmacological effects of a single dose of 300–800 mg of RDEA806 are equivalent to those exhibited by a 100 mg dose of Lesinurad [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 |
404.28
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CAS # |
878672-00-5
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Related CAS # |
Lesinurad sodium;1151516-14-1
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SMILES |
O=C(O)CSC1=NN=C(Br)N1C2=C3C=CC=CC3=C(C4CC4)C=C2
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Chemical Name |
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Synonyms |
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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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 (6.18 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
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 (6.18 mM) (saturation unknown) 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. 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 (6.18 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 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 |
*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. th> |
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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. |