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Lesinurad

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Chemical Structure| 878672-00-5 同义名 : 来司诺雷 ;RDEA594
CAS号 : 878672-00-5
货号 : A440574
分子式 : C17H14BrN3O2S
纯度 : 98%
分子量 : 404.281
MDL号 : MFCD22572730
存储条件：

粉末 Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(259.72 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 Lesinurad is a novel selective uric acid reabsorption inhibitor (SURI). Lesinurad is found to be a substrate for the kidney transporters organic anion transporter (OAT1) and OAT3 with Km values of 0.85 and 2 µM, respectively [1]. Lesinurad (RDEA594) functions as a URAT1 and OAT inhibitor, leading to increased proximal renal tubule urate excretion [2]. Lesinurad (RDEA594) serves as a potential uric acid-lowering agent by inhibiting uric acid reuptake. It also demonstrates favorable p450 profiles, inhibiting CYP2C9 and CYP2C8 with IC50 values of 14.4 μM and 16.2 μM, respectively. IC50 values for Lesinurad exceed 100 µM for CYP1A2, CYP2C19, and CYP2D6 [3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.47mL

0.49mL

0.25mL

12.37mL

2.47mL

1.24mL

24.74mL

4.95mL

2.47mL
参考文献

[1]Shen Z, et al. In Vitro and In Vivo Interaction Studies Between Lesinurad, a Selective Urate Reabsorption Inhibitor, and Major Liver or Kidney Transporters. Clin Drug Investig. 2016 Jun;36(6):443-52

[2]Sattui SE, et al. Treatment of hyperuricemia in gout: current therapeutic options, latest developments and clinical implications. Ther Adv Musculoskelet Dis. 2016 Aug;8(4):145-59.

[3]L.Yeh, et al. RDEA594, a potential uric acid lowering agent througn inhibition of uric acid reuptake ,shows better pharmacokinetics rhan its prodrug RDEA806. 2008 ACR/ARHP Annual Scientific Meeting, 24-29 October 2008, USA.