Home Transmembrane Transporters OAT inhibitor Verinurad (RDEA3170)

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Verinurad (RDEA3170) OAT inhibitor

Cat.No.S8736

Verinurad (RDEA3170) is a high-affinity inhibitor of the URAT1 transporter with an IC50 of 25 nM for inhibiting transport activity of human URAT1. It inhibits the related URAT1 homologs OAT4 and OAT1 with approximately 200-fold lower affinity compared to URAT1 with IC50 values of 5.9 µM and 4.6 µM, respectively.
Verinurad (RDEA3170) OAT inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 348.42

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Quality Control

Batch: S873601 DMSO]70 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.35%
99.35

Chemical Information, Storage & Stability

Molecular Weight 348.42 Formula

C20H16N2O2S

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 1352792-74-5 -- Storage of Stock Solutions

Synonyms N/A Smiles CC(C)(C(=O)O)SC1=C(C=NC=C1)C2=CC=C(C3=CC=CC=C32)C#N

Solubility

In vitro
Batch:

DMSO : 70 mg/mL (200.9 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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Mechanism of Action

Targets/IC50/Ki
URAT1 transporter [1]
(Cell-free assay)
25 nM
In vitro

Verinurad (RDEA3170) inhibited the transport activity of human URAT1 in a dose-dependent manner, at high potency with an IC50 of 25 nM. It inhibited the related URAT1 homologs OAT4 and OAT1 with approximately 200-fold lower affinity compared to URAT1 with IC50 values of 5.9 μM and 4.6 μM, respectively. Human URAT1 (IC50=0.025 μM) has a 1,640-fold higher affinity for this compound compared to rat URAT1(IC50 = 41 μM). It has a high potency for human URAT1, and residues 35, 365 and 481 all contribute to its affinity. Human URAT1 carrying a chimeric point mutation at position 365, in which human Phe-365 is replaced by rat Tyr-365 (human URAT1-F365Y or h-F365Y) has an IC50 of 4.0 μM, a significant 160-fold lower affinity relative to human URAT1. Meanwhile, rat URAT1 carrying the opposite point mutation (rat URAT1-Y365F or r-Y365F), had an IC50 of 2.9 μM, a significant 14-fold higher affinity compared to rat URAT1[1].
In vivo

In human, absorption of a single dose of Verinurad (RDEA3170) is rapid, and exposure (Cmax and AUC) increases with dose up to the maximum dose tested. Cmax is at 0.5-0.75 hours post dose in the fasted state, and is slightly delayed to 1.25 hours post dose in the fed state. The t1/2 is approximately 10-15 hours across doses. It was well tolerated at the doses studied. In the systemic circulation, this compound appeared to be a high clearance drug (CL/F ranged ~30-50 L/h) with extensive extravascular distribution. Renal excretion is limited to only ~2%–3% in the urine, suggesting that the majority is likely cleared in the liver via biotransformation to metabolites[2].
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04256629 Completed
Healthy Volunteers (Intended Indication: Chronic Kidney Disease)
AstraZeneca|Parexel
 March 3 2020 Phase 1
NCT02498652 Completed
Gout
Ardea Biosciences Inc.
 July 28 2015 Phase 2
NCT02336594 Completed
Gout
Ardea Biosciences Inc.
 November 2014 Phase 1

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