中文名：維立諾雷
英文名：Verinurad (RDEA3170)
純度：Moligand?，≥98%
貨號：V414145
Cas號：1352792-74-5
存儲溫度：-20°C儲存
運輸條件：超低溫運輸
產(chǎn)品介紹：
Information
Verinurad (RDEA3170) 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.
Targets
URAT1 transporter (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.
In vivo
In human, absorption of a single dose 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. Verinurad was well tolerated at the doses studied. In the systemic circulation, verinurad appeared to be a high clearance drug (CL/F ranged ~30-50 L/h) with extensive extravascular distribution. Renal excretion of verinurad is limited to only ~2%–3% in the urine, suggesting that the majority of verinurad is likely cleared in the liver via biotransformation to metabolites.
Cell Research(from reference)
Cell lines：HEK-293T cells?
Concentrations：0.1 nM-1 mM?
Incubation Time：5 min?
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關(guān)鍵字： CAS No.:1352792-74-5 ; C72401 ; SB19753 ; CCG-268013
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