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Verinurad (RDEA3170) OAT inhibitor

Name: Verinurad (RDEA3170)
Brand: Selleck Chemicals
SKU: S8736
Availability: InStock
Rating: 5 (2 reviews)

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.

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%

Cited in Nature Medicine for its top-tier quality
COA
NMR
SDS
Datasheet

99.35

Related Targets	CFTR CRM1 CD markers AChR Calcium Channel Sodium Channel Potassium Channel GABA Receptor TRP Channel ATPase
Other OAT Inhibitors	Dotinurad

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
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC(C)(C(=O)O)SC1=C(C=NC=C1)C2=CC=C(C3=CC=CC=C32)C#N

Mechanism of Action

Targets/IC₅₀/Ki	URAT1 transporter (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.
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.
References	[1] https://www.nature.com/articles/s41598-017-00706-7 [2] https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5511024/

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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