RDEA594 Lesinurad sodium

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Chemical Information

Product name：RDEA594 Lesinurad sodium	Purity：99.0% min
CAS NO：1151516-14-1	Solubility：DMSO : ≥ 26 mg/mL (61.00 mM)
Molecular Formula：C₁₇H₁₃BrN₃NaO₂S	Package：Package according to customer requirements
Molecular Weight：404.28096	Storage：Store at -20℃

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Remarks

Lesinurad is a novel selective uric acid reabsorption inhibitor (SURI). Lesinurad is determined to be a substrate for the kidney transporters organic anion transporter (OAT1) and OAT3 with Km values of 0.85 and 2 uM, respectively. Lesinurad (RDEA594) is a URAT1 and OAT inhibitor, which increases proximal renal tubule urate excretion. Lesinurad (RDEA594) is a potential uric acid lowering agent througn inhibition of uric acid reuptake, and exhibits favorable p450 profiles, inhibits CYP2C9 and CYP2C8 with IC50 of 14.4 uM and 16.2 uM, respectively. IC50s of Lesinurad are all above 100 uM for CYP1A2, CYP2C19,and CYP2D6.

Lesinurad sodium is a UART1 and OAT inhibitor, is determined to be a substrate for the kidney transporters OAT1 and OAT3 with K_m values of 0.85 and 2 µM, respectively.

References

[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.