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Lesinurad

CAS No. : 878672-00-5

MCE 站：Lesinurad

产品活性：Lesinurad 是一种 URAT1 和 OAT 抑制剂，用作肾转运蛋白OAT1 和OAT3 的底物，K_m值分别为 0.85 和 2 μM。

研究领域：Membrane Transporter/Ion Channel

作用靶点：URAT1

In Vitro: 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 K_m values of 0.85 and 2 ?M, 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 μM and 16.2 μM, respectively. IC₅₀s of Lesinurad are all above 100 ?M for CYP1A2, CYP2C19,and CYP2D6.

In Vivo: Lesinurad (RDEA594) shows better pharmacokinetics than its pro-drug RDEA806. The 100 mg dose of Lesinurad exhibits a phamacological effect in the range of that produced by 300 mg to 800 mg single doses of RDEA806.

相关产品：Drug Repurposing Compound Library Plus  |  FDA-Approved Drug Library Plus  |  FDA-Approved Drug Library Mini  |  Bioactive Compound Library Plus  |  Membrane Transporter/Ion Channel Compound Library  |  FDA-Approved Drug Library  |  Drug Repurposing Compound Library  |  Orally Active Compound Library  |  FDA Approved & Pharmacopeial Drug Library  |  URAT1 inhibitor 1

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