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Verinurad

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Chemical Structure| 1352792-74-5 同义名 : RDEA3170
CAS号 : 1352792-74-5
货号 : A287467
分子式 : C20H16N2O2S
纯度 : 99%+
分子量 : 348.418
MDL号 : MFCD28963965
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(301.36 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 URAT1 (urate transporter 1) is a transporter critical for renal reabsorption of urate. Inactivating mutations of URAT1 lead to high FEUA (fractional excretion of uric acid) and hypouricemia (abnormally low sUA (serum uric acid) levels). Verinurad inhibits the transport activity of human URAT1 in a dose-dependent manner, at high potency with an IC50 of 25 nM. And it’s currently under evaluation for the treatment of gout which is caused by elevated serum urate levels. Verinurad 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. Therefore, verinurad is highly specific for URAT1. Moreover, human URAT1 has a 1,640-fold higher affinity for verinurad compared to rat URAT1 (IC50 = 41 µM). Consistent with the in vitro inhibition of URAT1, treatment of healthy human volunteers with a single 40 mg dose of verinurad reduced the sUA by up to 60% and increased the FEUA in a dose-dependent manner with a half-maximal effective concentration in plasma of 22 nM[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.87mL

0.57mL

0.29mL

14.35mL

2.87mL

1.44mL

28.70mL

5.74mL

2.87mL
参考文献

[1]Shen Z, Gillen M, et al. Pharmacokinetics, pharmacodynamics, and tolerability of verinurad, a selective uric acid reabsorption inhibitor, in healthy adult male subjects. Drug Des Devel Ther. 2017 Jul 7;11:2077-2086.

[2]Tan PK, Liu S, et al. 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.

[3]Tan PK, Liu S, Gunic E, Miner JN. Discovery and characterization of verinurad, a potent and specific inhibitor of URAT1 for the treatment of hyperuricemia and gout. Sci Rep. 2017;7(1):665. Published 2017 Apr 6.