oat3

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.

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.

Indican (Indoxyl-β-D-glucoside) is a natural protective compound that is used to protect the liver.

Metronidazole (Metronidazol) is a synthetic nitroimidazole derivative with antiprotozoal and antibacterial activities.

Lesinurad sodium (RDEA594 sodium) is a selective inhibitor of uric acid reabsorption and is used in the study of cardiovascular diseases.

Diclofenac Acyl Glucuronide (Diclofenac glucuronide) is an intestinal metabolite that accelerates intestinal ulcers.

Cabotegravir sodium (GSK-1265744) is an orally active, membrane-permeable HIV integrase inhibitor (IC₅₀ = 2.5 μM) and also an OAT1/OAT3 inhibitor (IC₅₀ = 0.81/0.41 μM). It inhibits HIV replication and may be used in AIDS research.

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).

Quinaprilat is an orally active ACE inhibitor, the active metabolite of quinapril, and a substrate for OAT3. It blocks the conversion of angiotensin I to angiotensin II, exhibiting antihypertensive activity.

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].

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).

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

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.

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].

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].

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].

Obtusichromoneside C is a chromone C-glycoside identified in the seeds of Cassia obtusifolia. It modulates substance transport by inhibiting the uptake of substrates by specific transport proteins, such as OAT3 and OATP1B3. This compound shows potential for use in drug transport research.