organic anion transporter

Digitoxin (Digitoxinum) 是Na+ K+-ATPase 有效抑制剂, EC50 值为0.78 μM。

Dimesna (BNP-7787) 是一种二硫代乙烷磺酸盐的合成衍生物，具有泌尿保护特性。

Morinidazole 具有抗菌活性，可用于厌氧菌引起的阑尾炎、盆腔炎等细菌感染研究。

Verinurad (RDEA3170) 是一种有效的、特异性的URAT1抑制剂，IC50为 25 nM。

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。

SOAT-IN-1 (compound 40) 作为钠依赖性有机阴离子转运体 (sodium-dependent organic anion transporter (SOAT)) 的有效选择性抑制剂，其对SOAT的IC50为1.6 µM，对NTCP的IC50为14.3 µM。

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)

Estradiol 17-(β-D-glucuronide) (E217G) is an estrogen metabolite formed in the liver and subsequently excreted in bile.1It acts as a substrate of the multidrug resistance protein 2 (MRP2; Km= 75 μM), and through MRP2-mediated transport, functions as a cholestatic agent, decreasing bile flow.1,2In addition to binding to the MRP2 transport site, E217G has been shown to bind to an allosteric site that through positive cooperativity activates its own transportviaMRP2 and the transport of other MRP2 substrates, including the non-cholestatic estrogen metabolite, estradiol 3-(β-D-glucuronide) .2,3E217G has also been reported to be transported by MDR1, MRP1, MRP3, MRP4, MRP7, ABCG2 (a breast cancer resistance protein transporter), and the rat organic anion-transporting polypeptides 1-4.2 1.Loe, D.W., Almquist, K.C., Cole, S.P., et al.ATP-dependent 17β-estradiol 17-(β-D-glucuronide) transport by multidrug resistance protein (MRP). Inhibition by cholestatic steroidsThe Journal of Biological Chemisty271(16)9683-9689(1996) 2.Gerk, P.M., Li, W., and Vore, M.Estradiol 3-glucuronide is transported by the multidrug resistance-associated protein 2 but does not activate the allosteric site bound by estradiol 17-glucuronideDrug Metabolism and Disposition32(10)1139-1145(2004) 3.Gerk, P.M., Li, W., Megaraj, W., et al.Human multidrug resistance protein 2 transports the therapeutic bile salt tauroursodeoxycholateJournal of Pharmacology and Experimental Therapeutics320(2)893-899(2007)

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.