Date published: 2025-9-18

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OAT3 Inhibitors

OAT3 inhibitors encompass a variety of chemicals that indirectly modulate the function and activity of OAT3, a transporter protein primarily involved in the renal excretion of organic anions, including various drugs and metabolites. These inhibitors function by targeting renal excretion pathways and drug metabolism processes crucial for OAT3's role in the kidneys. For instance, Probenecid and Furosemide, a uricosuric agent and a loop diuretic respectively, inhibit renal tubular secretion and ion transport, thereby potentially affecting OAT3's function in drug excretion. NSAIDs like Indomethacin, Ibuprofen, Ketoprofen, and Diclofenac can influence renal anion transport, potentially inhibiting OAT3's activity in the excretion of organic anions. Other inhibitors, such as Cimetidine, Losartan, and Methotrexate, known for their roles in affecting histamine receptor activity, angiotensin II receptor antagonism, and as an antimetabolite, respectively, may indirectly impact OAT3 by altering renal drug excretion pathways. Antibiotics like Ceftriaxone, statins such as Atorvastatin, and antidiabetic drugs like Glyburide, with their interaction in renal transport mechanisms, represent another approach to modulating OAT3 activity.

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