| Description |
UT-B-IN-1 (UTBINH-14) is a reversible, competitive and selective urea transporter-B (UT-B) inhibitor with IC50 values of 10 and 25 nM for human and mouse UT-B, respectively. UT-B-IN-1 shows low toxicity and high selectivity for UT-B over UT-A isoforms. UT-B-IN-1 increases urine output and reduces urine osmolality of mice. UT-B-IN-1 can be used for diuretic mechanism research[1].
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| Related Catalog |
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| Target |
IC50: 10 nM (human UT-B); 25 nM (mouse UT-B)[1]
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| In Vitro |
UT-B-IN-1 (1-1000 nM) 抑制尿素预载红细胞的尿素外排，IC50 值为 26.7 nM[1]。 UT-B-IN-1 抑制 AQP1-null 红细胞的水运输[1]。 UT-B-IN-1 (0-10 μM；24 h) 对 MDCK 细胞无细胞毒性[1]。 Cell Cytotoxicity Assay[1] Cell Line: Madin-Darby canine kidney (MDCK) cell line Concentration: 0-10 μM Incubation Time: 24 hours Result: Exhibited no cytotoxic effect to MDCK cells.
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| In Vivo |
UT-B-IN-1 (300 μg；腹腔注射，1 次) 在自由取水和进食的小鼠中，增加排尿量并降低尿液渗透性[1]。 Animal Model: Male mice (wild-type or UT-B knockout)[1] Dosage: 300 μg Administration: Intraperitoneal injection, 300 μg, once Result: Reduced urine osmolality and urea concentration in wild-type mice with V2-receptor agonist dDAVP injection. Increased urine volume and reduced urine osmolality and urea concentration in mice with free access to food and water but without dDAVP.
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| References |
[1]. Yao C, et al. Triazolothienopyrimidine inhibitors of urea transporter UT-B reduce urine concentration. J Am Soc Nephrol. 2012 Jul;23(7):1210-20.
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