8
2
Cat. No. | Product Name | Target | Signaling Pathways |
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T6875 |
Lesinurad
RDEA594,雷西那德,来司诺雷 |
OAT | Membrane transporter/Ion channel |
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。 | |||
T6098 |
Cabotegravir
GSK744,GSK-1265744,卡博特韦,S/GSK1265744 |
HIV Protease | Microbiology/Virology; Proteases/Proteasome |
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。 | |||
T69889 | JBP485 | ||
JBP485 is an inhibitor of renal transporters OAT1 and OAT3. JBP485 is an antihepatitis agent as a substrate for intestinal PEPT1. | |||
T35721 |
4’-hydroxy Trazodone
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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 poten... | |||
T27275 | Epaminurad | ||
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。 | |||
T74729 |
18β-Glycyrrhetyl-3-O-sulfate
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18β-Glycyrrhetyl-3-O-sulfate(Glycyrrhetic acid 3-O-(hydrogen sulfate))是一种对2型11β-羟基类固醇脱氢酶(11β-HSD2)具有高效抑制作用的化合物,其在大鼠肾微粒体中的IC50值为0.10 µM。作为Glycyrrhetinic acid (GA)的重要代谢产物,18β-Glycyrrhetyl-3-O-sulfate同时也是有机阴离子转运蛋白(OAT)1和OAT3的底物。此外,该化合物展示出抗炎活性,并可能用于假性醛固酮增多症的研究领域。 | |||
T70313 | Indoxyl Sulfate-d5 potassium salt | ||
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). ... | |||
T21301 |
Lesinurad sodium
Lesinurad,RDEA 594,RDEA-594,RDEA594 |
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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. |
Cat. No. | Product Name | Target | Signaling Pathways |
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T81629 |
OAT1/3-IN-2
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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。 | |||
T81630 |
OAT1/3-IN-1
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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。 |