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OAT-1441 is a hAMCase inhibitor.

OAT-177 is a potent, selective, orally active acidic mammalian chitinase (AMCase) inhibitor.

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).

5-Fluoromethylornithine dihydrochloride (5-FMOrn dihydrochloride) is a selective inhibitor of L-Ornithine:2-oxoacid aminotransferase (OAT) and a specific inactivator of OAT, which can be used to study metabolic diseases and neurological diseases.

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].

MFH290 is a novel cysteine (Cys)-directed covalent inhibitor of CDK12/13. MFH290 forms a covalent bond with Cys-1039 of CDK12, exhibits excellent kinome selectivity, inhibits the phosphorylation of serine-2 in the C-terminal domain (CTD) of RNA-polymerase II (Pol II), and reduces the expression of key DNA damage repair genes. Importantly, these effects were demonstrated to be CDK12-dependent as mutation of Cys-1039 rendered the kinase refractory to MFH290 and restored Pol II CTD phosphorylation and DNA damage repair gene expression. Consistent with its effect on DNA damage repair gene expression, MFH290 augments the antiproliferative effect of the PARP inhibitor olaparib.

P7170 is an anti-cancer agent active as an mTORC1/C2 and activin receptor-like kinase 1 (ALK1) inhibitor.

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.

Lingdolinurad is a uric acid transporter protein inhibitor targeting hURAT1 for the study of hyperuricemia or gout.

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.

Benzarone (Benzarona) is a potent inhibitor of human uric acid transporter 1 (URAT1, IC50 = 2.8 μM in oocyte). Benzarone lowers the level of uric acid serum.

Verinurad (RDEA3170) (RDEA3170) is an organic anion transporter URAT1 (SLC22A12) inhibitor for the treatment of gout and hyperuricemia.

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

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].

URAT1 inhibitor 1 (1g) is a potent inhibitor of uric acid transporter 1 (URAT1) with an IC50 of 32 nM, and has potential therapeutic applications for treating hyperuricemia associated with gout.

Dotinurad ((3,5-dichloro-4-hydroxyphenyl)(1,1-dioxidobenzo[d]thiazol-3(2H)-yl)methanone) is a potent agent of uricosuric (IC50: 3.6 μM for uric acid).

Cyazofamid functions as a fungicide by impairing the production of ATP. It inhibits Organic Cation Transporter 3 (OCT3) and OAT1 with IC50 values of 1.54 and 17.3 μM, respectively.

URAT1-IN-14 is a potent and orally active inhibitor of uric acid transporter 1 (URAT1). It demonstrates an IC50 value of 0.72 μM for inhibiting human URAT1 in HEK293 cells and exhibits low cytotoxicity in Hep-G2 cells. URAT1-IN-14 reduces uric acid levels in a hyperuricemia mouse model and is applicable in research on hyperuricemia and gout.

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

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].

Fraxin (Fraxoside) is a glucoside of fraxetin.

Ruzinurad (WO2020088641, compound I) is a potent URAT1 inhibitor, exhibiting high selectivity. This compound shows great promise for investigating hyperuricemia.

URAT1 inhibitor 3 is a potent, orally active, selective inhibitor of URAT1 (IC50 = 0.8 nM) demonstrating urate-lowering efficacy, suitable for research in gout and hyperuricemia [1].