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Verinurad (RDEA3170)

Alias: RDEA-3170; RDEA3170; RDEA 3170
Cat No.:V3308 Purity: ≥98%
Verinurad (formerly known as RDEA-3170; RDEA3170) is a novel, highly potent and specificURAT1(Urate transporter 1) inhibitor with anti-hyperuricemic effects.
Verinurad (RDEA3170)
Verinurad (RDEA3170) Chemical Structure CAS No.: 1352792-74-5
Product category: URAT1
This product is for research use only, not for human use. We do not sell to patients.
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Top Publications Citing lnvivochem Products
InvivoChem's Verinurad (RDEA3170) has been cited by 1 publication
Purity & Quality Control Documentation

Purity: ≥98%

Product Description

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.

Biological Activity I Assay Protocols (From Reference)
Targets

IC50: 25 nM (URAT1)[1]

ln Vitro
With an IC50 of 25 nM, verinurad exhibits strong efficacy and dose-dependent inhibition of human URAT1's transport activity [1].
References

[1]. Discovery and characterization of verinurad, a potent and specific inhibitor of URAT1 for the treatment of hyperuricemia and gout. Sci Rep. 2017 Apr 6;7(1):665.

Additional Infomation
Verinurad has been used in trials studying the basic science and treatment of Gout, Gout and Hyperuricemia, and Gout and Asymptomatic Hyperuricemia.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C20H16N2O2S
Molecular Weight
348.42
Exact Mass
348.093
Elemental Analysis
C, 68.95; H, 4.63; N, 8.04; O, 9.18; S, 9.20
CAS #
1352792-74-5
Related CAS #
1352792-74-5
PubChem CID
54767229
Appearance
White to off-white solid powder
Density
1.3±0.1 g/cm3
Boiling Point
566.7±50.0 °C at 760 mmHg
Flash Point
296.5±30.1 °C
Vapour Pressure
0.0±1.6 mmHg at 25°C
Index of Refraction
1.692
LogP
3.77
Hydrogen Bond Donor Count
1
Hydrogen Bond Acceptor Count
5
Rotatable Bond Count
4
Heavy Atom Count
25
Complexity
541
Defined Atom Stereocenter Count
0
SMILES
CC(C)(SC1=C(C2=C3C=CC=CC3=C(C#N)C=C2)C=NC=C1)C(O)=O
InChi Key
YYBOLPLTQDKXPM-UHFFFAOYSA-N
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)
Chemical Name
2-((3-(4-cyanonaphthalen-1-yl)pyridin-4-yl)thio)-2-methylpropanoic acid
Synonyms
RDEA-3170; RDEA3170; RDEA 3170
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO:≥ 30mg/mL
Water:N/A
Ethanol:N/A
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.

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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.
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 corn oil and mix evenly.


 (Please use freshly prepared in vivo formulations for optimal results.)
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.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
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  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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.

Biological Data
  • Verinurad (RDEA3170)


    Verinurad is highly potent and specific for human URAT1.2017 Apr 6;7(1):665.

  • Verinurad (RDEA3170)

    Phe-365 of human URAT1 is important for affinity for verinurad.2017 Apr 6;7(1):665.

  • Verinurad (RDEA3170)

    Human URAT1 Ser-35 and Phe-365 cooperate to enhance urate affinity.2017 Apr 6;7(1):665.

  • Verinurad (RDEA3170)


    Each URAT1 inhibitor has a distinct profile of potencies for URAT1 mutants.2017 Apr 6;7(1):665.

  • Verinurad (RDEA3170)


    A novel URAT1 binding assay replicates the results of inhibition of URAT1 activity.2017 Apr 6;7(1):665.

  • Verinurad (RDEA3170)

    Inhibitors bind to the same binding site on URAT1.

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