oat1

Epaminurad HCl 是一种可口服且具有特异性和高效性的尿酸转运体 1 (URAT1 ) 抑制剂（ Ki：57 nM），对 OAT1 和 OAT3 (有机阴离子转运体)有部分抑制作用。Epaminurad HCl 是一种促尿酸排泄剂，可用于预防和治疗痛风和高尿酸血症。

Lesinurad (RDEA594) 是URAT1和OAT 抑制剂。Lesinurad 用作肾转运蛋白OAT1 和OAT3 的底物，Km 分别为 0.85 和 2 μM。

Indican (Indoxyl-β-D-glucoside) 是吲哚酚的一种糖苷，染料靛蓝和靛玉红的前体。它的主要代谢物是硫酸吲哚酚 (IS)。其中 IS 是尿毒症毒素，是有机阴离子转运蛋白1 (OAT 1)、OAT 3 和多药耐药相关蛋白4 (MRP 4) 的底物 抑制剂。

OAT1 3-IN-2（化合物8）是一种针对OAT1和OAT3的双重抑制剂。该化合物能够以10 μM的浓度逆转Cys-Hg对HEK-OAT1细胞的毒害作用，并可能对肾脏具有保护效应。OAT1 3-IN-2适用于研究汞导致的肾脏损伤。

OAT1 3-IN-1（化合物7）是针对OAT1和OAT3的双重抑制剂。该化合物能逆转Cys-Hg（10 μM）对HEK-OAT1细胞引起的毒害，表明其对肾脏有潜在的保护效应。OAT1 3-IN-1适合用于探究汞引起的肾脏损伤机制研究。

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.

OAT-1441 is a hAMCase inhibitor.

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

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

Cabotegravir (S GSK1265744) 是一种HIV 整合酶抑制剂，可研究艾滋病。它抑制OAT1 和OAT3，IC50值为 0.81 和0.41 μM。

Cyazofamid 抑制细菌中的 ATP 生成能力来发挥其杀菌效果。此外，该化合物对有机阳离子转运蛋白 3 (OCT3) 和 OAT1 的抑制作用表现出了显著的差异，其 IC50 值分别是 1.54 μM 和 17.3 μM。

Lesinurad sodium (RDEA594 sodium) 是一种具有选择性的尿酸重吸收抑制剂，可用于研究心血管疾病。

Diclofenac Acyl Glucuronide (Diclofenac glucuronide) 是一种肠道代谢物，可加速肠道溃疡。

Epaminurad (UR-1102) 是一种口服有效的和选择性的URAT1(尿酸转运体 1) 抑制剂，其Ki 为 0.057 μM。Epaminurad 适度地抑制OAT1和OAT3(有机阴离子转运体)。Epaminurad 是一种促尿酸排泄剂。Epaminurad 可用于痛风和高尿酸血症的研究。

4’-hydroxy Trazodone is a metabolite of the antidepressant and sedative trazodone.1It is an inhibitor of organic anion transporter 3 (OAT3; Ki= 16.9 μM) and is selective for OAT3 over OAT1 (Ki= >200 μM).2 1.Yamato, C., Takahashi, T., Fujita, T., et al.Studies on metabolism of trazodone, II. Metabolic fate after intravenous administration and effects on liver microsomal drug-metabolizing enzymes in ratsXenobiotica4(12)765-777(1974) 2.Zou, L., Matsson, P., Stecula, A., et al.Drug metabolites potently inhibit renal organic anion transporters, OAT1 and OAT3J. Pharm. Sci.110(1)347-353(2021)

KPH2f 是一种安全、口服有效的 URAT1 GLUT9双抑制剂，对 URAT1和 GLUT9 的 IC50分别为 0.24 μM 和 9.37 μM。KPH2f 对 OAT1 和 ABCG2 几乎没有影响 (IC50分别为 32.14 和 26.74 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.