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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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Purity: ≥98%
Verinurad (formerly known as RDEA-3170; RDEA3170) is a novel, highly potent and specific URAT1 (Urate transporter 1) inhibitor with anti-hyperuricemic effects. It inhibits URAT1 with an IC50 of 25 nM and is currently under clinical trials for treating gout. High affinity inhibition of uric acid transport requires URAT1 residues Cys-32, Ser-35, Phe-365 and Ile-481. Unlike other available uricosuric agents, the requirement for Cys-32 is unique to verinurad. Two of these residues, Ser-35 and Phe-365, are also important for urate transport kinetics. A URAT1 binding assay using radiolabeled verinurad revealed that distinct URAT1 inhibitors benzbromarone, sulfinpyrazone and probenecid all inhibit verinurad binding via a competitive mechanism. However, mutations made within the predicted transporter substrate channel differentially altered the potency for individual URAT1 inhibitors. Overall, the results suggest that URAT1 inhibitors bind to a common site in the core of the transporter and sterically hinder the transit of uric acid through the substrate channel, albeit with vastly different potencies and with differential interactions with specific URAT1 amino acids.
Targets |
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ln Vitro |
With an IC50 of 25 nM, verinurad exhibits strong efficacy and dose-dependent inhibition of human URAT1's transport activity [1].
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Additional Infomation |
Verinurad has been used in trials studying the basic science and treatment of Gout, Gout and Hyperuricemia, and Gout and Asymptomatic Hyperuricemia.
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Molecular Formula |
C20H16N2O2S
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Molecular Weight |
348.42
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Exact Mass |
348.093
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Elemental Analysis |
C, 68.95; H, 4.63; N, 8.04; O, 9.18; S, 9.20
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CAS # |
1352792-74-5
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Related CAS # |
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PubChem CID |
54767229
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Appearance |
White to off-white solid powder
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Density |
1.3±0.1 g/cm3
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Boiling Point |
566.7±50.0 °C at 760 mmHg
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Flash Point |
296.5±30.1 °C
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Vapour Pressure |
0.0±1.6 mmHg at 25°C
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Index of Refraction |
1.692
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LogP |
3.77
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Hydrogen Bond Donor Count |
1
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Hydrogen Bond Acceptor Count |
5
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Rotatable Bond Count |
4
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Heavy Atom Count |
25
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Complexity |
541
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Defined Atom Stereocenter Count |
0
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SMILES |
CC(C)(SC1=C(C2=C3C=CC=CC3=C(C#N)C=C2)C=NC=C1)C(O)=O
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InChi Key |
YYBOLPLTQDKXPM-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C20H16N2O2S/c1-20(2,19(23)24)25-18-9-10-22-12-17(18)16-8-7-13(11-21)14-5-3-4-6-15(14)16/h3-10,12H,1-2H3,(H,23,24)
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Chemical Name |
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Synonyms |
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HS Tariff Code |
2934.99.9001
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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 (7.18 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension 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 (7.18 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 (7.18 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 | 2.8701 mL | 14.3505 mL | 28.7010 mL | |
5 mM | 0.5740 mL | 2.8701 mL | 5.7402 mL | |
10 mM | 0.2870 mL | 1.4350 mL | 2.8701 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.
Verinurad is highly potent and specific for human URAT1.Sci Rep.2017 Apr 6;7(1):665. th> |
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Phe-365 of human URAT1 is important for affinity for verinurad.Sci Rep.2017 Apr 6;7(1):665. td> |
Human URAT1 Ser-35 and Phe-365 cooperate to enhance urate affinity.Sci Rep.2017 Apr 6;7(1):665. td> |
Each URAT1 inhibitor has a distinct profile of potencies for URAT1 mutants.Sci Rep.2017 Apr 6;7(1):665. th> |
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A novel URAT1 binding assay replicates the results of inhibition of URAT1 activity.Sci Rep.2017 Apr 6;7(1):665. td> |
Inhibitors bind to the same binding site on URAT1. td> |