[CAS NO. 1352792-74-5] Verinurad (RDEA3170)
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PRODUCTS SPECIFICATIONS [1352792-74-5]
Catalog
SLK-S8736
Brand
Selleck
CAS
1352792-74-5
DESCRIPTION [1352792-74-5]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 348.42 |
| Molecular Formula | C20H16N2O2S |
| SMILES | CC(C)(SC1=C(C2=C3C=CC=CC3=C(C#N)C=C2)C=NC=C1)C(O)=O |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
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 |
| 50 mM | 0.0574 mL | 0.2870 mL | 0.5740 mL |
Description
Verinurad (RDEA3170) is a high-affinity inhibitor of the with an 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.
Targets
| URAT1 transporter [1] (Cell-free assay) |
| 25 nM |
In vitro
Verinurad inhibited the transport activity of human URAT1 in a dose-dependent manner, at high potency with an IC50 of 25 nM. Verinurad 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 verinurad compared to rat URAT1(IC50 = 41 μM). Verinurad has a high potency for human URAT1, and residues 35, 365 and 481 all contribute to verinurad 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.
References
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