oat3

Lesinurad (RDEA594) is a selective inhibitor of uric acid reabsorption which is used in combination with other agents in the therapy of gout. Lesinurad has had a limited clinical use but has not been associated with serum enzyme elevations during therapy or with instances of clinically apparent liver injury.

Cabotegravir (S/GSK1265744) (GSK744, GSK1265744) is a long-acting HIV integrase inhibitor and inhibits the HIV-1 integrase catalyzed strand transfer reaction (IC50: 3.0 nM).

Epaminurad HCl is a URAT1 inhibitor with partial inhibition of OAT1 and OAT3 (organic anion transporters).Epaminurad HCl is a pro-uric acid excretory agent used for the prevention and treatment of gout and hyperuricemia.

UNC569, the first small-molecule MER inhibitor, inhibits Mer activation and downstream signaling through ERK1/2 and AKTwith. UNC569 shows efficacy against acute lymphoblastic leukemia in vitro and in vivo.

OAT1 3-IN-2 (compound 8) is a dual inhibitor of OAT1 and OAT3, demonstrating potential protective effects against Cys-Hg toxicity in HEK-OAT1 cells (10 μM) and may safeguard renal function. This compound is useful for investigating mercury-induced nephrotoxicity [1].

4’-Hydroxy Trazodone, a metabolite of the antidepressant and sedative trazodone, is an inhibitor of organic anion transporter 3 (OAT3; Ki = 16.9 μM) and is selective for OAT3 over OAT1 (Ki > 200 μM).

OAT1 3-IN-1 (compound 7), a dual inhibitor of OAT1 and OAT3, mitigates Cys-Hg toxicity in HEK-OAT1 cells at 10 μM and offers potential kidney protection. This compound is used in the investigation of mercury-induced renal damage [1].

18β-Glycyrrhetyl-3-O-sulfate (Glycyrrhetic acid 3-O-(hydrogen sulfate)), a major metabolite of Glycyrrhetinic acid (GA), is a potent inhibitor of type 2 11β-hydroxysteroid dehydrogenase (11β-HSD2) with an IC50 value of 0.10 µM in rat kidney microsome assays. This compound is a substrate for organic anion transporters (OAT) 1 and OAT3, exhibits anti-inflammatory properties, and holds potential for research into pseudohyperaldosteronism [1] [2].

Indoxyl sulfate-d5 is intended for use as an internal standard for the quantification of indoxyl sulfate by GC- or LC-MS. Indoxyl sulfate is a uremic toxin and a metabolite of tryptophan. It is formed via sulfation of indole, an intermediate generated from tryptophan by intestinal bacteria, by the sulfotransferase (SULT) isoform 1A1 variant 2 (SULT1A1*2) in the liver. Indoxyl sulfate activates the aryl hydrocarbon receptor (AhR) in HepG2 40/6 hepatoma cells (EC50 = 12.1 nM in a reporter assay). It also inhibits the organic anion transporter (OAT) isoforms OAT1 and OAT3 (Kis = 34.2 and 74.4 µM, respectively for the rat transporters) in S2 proximal tubule cells. Indoxyl sulfate (0.2 and 1 mM) increases superoxide anion and nitric oxide levels in isolated human mononuclear blood cells. It increases serum creatinine and blood urea nitrogen (BUN) levels in the 5/6 nephrectomized rat model of chronic renal failure when administered at a dose of 50 mg/kg.

JBP485 is an inhibitor of renal transporters OAT1 and OAT3. JBP485 is an antihepatitis agent as a substrate for intestinal PEPT1.

Epaminurad (UR-1102) is an orally active, potent, and selective URAT1 (urate transporter 1) inhibitor with a Ki of 0.057 μM, and it inhibits OAT1 and OAT3 (organic anion transporter) modestly. Epaminurad is a uricosuric agent used for research on gout and hyperuricemia [1].

Indoxyl sulfate is a metabolite of tryptophan, showing adverse effects on bones and the central nervous system, having been most frequently implicated as a contributor to renal disease progression and vascular disease